Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship (English)
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In:
Journal of Enzyme Inhibition and Medicinal Chemistry
;
34
, 1
;
577-588
;
2019
- Article (Journal) / Electronic Resource
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Title:Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
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Contributors:Proença, Carina ( author ) / Freitas, Marisa ( author ) / Ribeiro, Daniela ( author ) / Tomé, Sara M. ( author ) / Oliveira, Eduardo F. T. ( author ) / Viegas, Matilde F. ( author ) / Araújo, Alberto N. ( author ) / Ramos, Maria J. ( author ) / Silva, Artur M. S. ( author ) / Fernandes, Pedro A. ( author )
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Published in:Journal of Enzyme Inhibition and Medicinal Chemistry ; 34, 1 ; 577-588
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Publisher:
- New search for: Taylor & Francis
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Publication date:2019-01-01
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Size:12 pages
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ISSN:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Keywords:
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Source:
Table of contents – Volume 34, Issue 1
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 1
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Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracerElie, Jonathan / Vercouillie, Johnny / Arlicot, Nicolas / Lemaire, Lucas / Bidault, Rudy / Bodard, Sylvie / Hosselet, Christel / Deloye, Jean-Bernard / Chalon, Sylvie / Emond, Patrick et al. | 2019
- 8
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Phosphonate inhibitors of West Nile virus NS2B/NS3 proteaseSkoreński, Marcin / Milewska, Aleksandra / Pyrć, Krzysztof / Sieńczyk, Marcin / Oleksyszyn, Józef et al. | 2019
- 15
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Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agentsHu, Yuheng / Wang, Bing / Yang, Jie / Liu, Teng / Sun, Jie / Wang, Xiaojing et al. | 2019
- 31
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Refining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoformsMagalhães, Joana / Franko, Nina / Annunziato, Giannamaria / Pieroni, Marco / Benoni, Roberto / Nikitjuka, Anna / Mozzarelli, Andrea / Bettati, Stefano / Karawajczyk, Anna / Jirgensons, Aigars et al. | 2019
- 44
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iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancerCilibrizzi, Agostino / Floresta, Giuseppe / Abbate, Vincenzo / Giovannoni, Maria Paola et al. | 2019
- 51
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Determination of the inhibitory effects of N-methylpyrrole derivatives on glutathione reductase enzymeKocaoğlu, Esma / Talaz, Oktay / Çavdar, Hüseyin / Şentürk, Murat / Supuran, Claudiu T. / Ekinci, Deniz et al. | 2019
- 55
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From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitorsMassari, Serena / Corona, Angela / Distinto, Simona / Desantis, Jenny / Caredda, Alessia / Sabatini, Stefano / Manfroni, Giuseppe / Felicetti, Tommaso / Cecchetti, Violetta / Pannecouque, Christophe et al. | 2019
- 75
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Assessment of the antiproliferative and apoptotic roles of sulfonamide carbonic anhydrase IX inhibitors in HeLa cancer cell lineKoyuncu, Ismail / Gonel, Ataman / Durgun, Mustafa / Kocyigit, Abdurrahim / Yuksekdag, Ozgur / Supuran, Claudiu T. et al. | 2019
- 87
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Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3Sciú, M. Lourdes / Sebastián-Pérez, Victor / Martinez-Gonzalez, Loreto / Benitez, Rocio / Perez, Daniel I. / Pérez, Concepción / Campillo, Nuria E. / Martinez, Ana / Moyano, E. Laura et al. | 2019
- 97
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Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moietyAbdel-Maksoud, Mohammed S. / El-Gamal, Mohammed I. / Gamal El-Din, Mahmoud M. / Oh, Chang Hyun et al. | 2019
- 110
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Synthesis and cytotoxic activities of novel copper and silver complexes of 1,3-diaryltriazene-substituted sulfonamidesCanakci, Dilek / Koyuncu, Ismail / Lolak, Nabih / Durgun, Mustafa / Akocak, Suleyman / Supuran, Claudiu T. et al. | 2019
- 117
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The carbonic anhydrase IX inhibitor SLC-0111 sensitises cancer cells to conventional chemotherapyAndreucci, Elena / Ruzzolini, Jessica / Peppicelli, Silvia / Bianchini, Francesca / Laurenzana, Anna / Carta, Fabrizio / Supuran, Claudiu T. / Calorini, Lido et al. | 2019
- 124
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Synthesis of novel 6,7-dimethoxy-4-anilinoquinolines as potent c-Met inhibitorsZhang, Qing-Wen / Ye, Zi-Dan / Shen, Chang / Tie, Hong-Xia / Wang, Lei / Shi, Lei et al. | 2019
- 134
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Computational screening of chalcones acting against topoisomerase IIα and their cytotoxicity towards cancer cell linesSangpheak, Kanyani / Mueller, Monika / Darai, Nitchakan / Wolschann, Peter / Suwattanasophon, Chonticha / Ruga, Ritbey / Chavasiri, Warinthon / Seetaha, Supaporn / Choowongkomon, Kiattawee / Kungwan, Nawee et al. | 2019
- 144
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HPLC–UV assay for the evaluation of inhibitors of plasma amine oxidase using crude bovine plasmaMergemeier, Kira / Galster, Florian / Lehr, Matthias et al. | 2019
- 150
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Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitorsGao, Cheng-Zhi / Dong, Wei / Cui, Zhi-Wen / Yuan, Qiong / Hu, Xia-Min / Wu, Qing-Ming / Han, Xianlin / Xu, Yao / Min, Zhen-Li et al. | 2019
- 163
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Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapyDgachi, Youssef / Martin, Hélène / Malek, Rim / Jun, Daniel / Janockova, Jana / Sepsova, Vendula / Soukup, Ondrej / Iriepa, Isabel / Moraleda, Ignacio / Maalej, Emna et al. | 2019
- 171
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Repurposing existing drugs: identification of irreversible IMPDH inhibitors by high-throughput screeningSarwono, Albertus Eka Yudistira / Mitsuhashi, Shinya / Kabir, Mohammad Hazzaz Bin / Shigetomi, Kengo / Okada, Tadashi / Ohsaka, Fumina / Otsuguro, Satoko / Maenaka, Katsumi / Igarashi, Makoto / Kato, Kentaro et al. | 2019
- 179
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Carbonic anhydrase 12 mutation modulates membrane stability and volume regulation of aquaporin 5Hwang, Soyoung / Kang, Jung Yun / Kim, Min Jae / Shin, Dong Min / Hong, Jeong Hee et al. | 2019
- 189
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Identification and characterization of the α-CA in the outer membrane vesicles produced by Helicobacter pyloriRonci, Maurizio / Del Prete, Sonia / Puca, Valentina / Carradori, Simone / Carginale, Vincenzo / Muraro, Raffaella / Mincione, Gabriella / Aceto, Antonio / Sisto, Francesca / Supuran, Claudiu T. et al. | 2019
- 196
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Synthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitorsBerwaldt, Gabriele A. / Gouvêa, Daniela P. / da Silva, Daniel S. / das Neves, Adriana M. / Soares, Mayara S. P. / Azambuja, Juliana H. / Siqueira, Geonir M. / Spanevello, Roselia M. / Cunico, Wilson et al. | 2019
- 203
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Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancersWang, Caolin / Xu, Shan / Peng, Liang / Zhang, Bingliang / Zhang, Hong / Hu, Yingying / Zheng, Pengwu / Zhu, Wufu et al. | 2019
- 218
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Comparison of blood carbonic anhydrase activity of athletes performing interval and continuous running exercise at high altitudeTas, Murat / Senturk, Esra / Ekinci, Deniz / Demirdag, Ramazan / Comakli, Veysal / Bayram, Metin / Akyuz, Murat / Senturk, Murat / Supuran, Claudiu T. et al. | 2019
- 224
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(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activatorsRami, Marouan / Winum, Jean-Yves / Supuran, Claudiu T. / Melnyk, Patricia / Yous, Saïd et al. | 2019
- 230
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Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivativesPopovici, Lacramioara / Amarandi, Roxana-Maria / Mangalagiu, Ionel I. / Mangalagiu, Violeta / Danac, Ramona et al. | 2019
- 244
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Inhibition of bacterial α-, β- and γ-class carbonic anhydrases with selenazoles incorporating benzenesulfonamide moietiesAngeli, Andrea / Pinteala, Mariana / Maier, Stelian S. / Del Prete, Sonia / Capasso, Clemente / Simionescu, Bogdan C. / Supuran, Claudiu T. et al. | 2019
- 250
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Discovery of cyanopyridine scaffold as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors through virtual screening and preliminary hit optimisationXu, Xi / Ren, Jie / Ma, Yinghe / Liu, Hongting / Rong, Quanjin / Feng, Yifan / Wang, Yameng / Cheng, Yu / Ge, Ruijia / Li, Zhiyu et al. | 2019
- 264
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Hydroxyl-substituted double Schiff-base condensed 4-piperidone/cyclohexanones as potential anticancer agents with biological evaluationZhang, Lianshuang / Chen, Qin / Hou, Guige / Zhao, Wei / Hou, Yun et al. | 2019
- 272
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Prostate cancer cells and exosomes in acidic condition show increased carbonic anhydrase IX expression and activityLogozzi, Mariantonia / Capasso, Clemente / Di Raimo, Rossella / Del Prete, Sonia / Mizzoni, Davide / Falchi, Mario / Supuran, Claudiu T. / Fais, Stefano et al. | 2019
- 279
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A comprehensive review on tyrosinase inhibitorsZolghadri, Samaneh / Bahrami, Asieh / Hassan Khan, Mahmud Tareq / Munoz-Munoz, J. / Garcia-Molina, F. / Garcia-Canovas, F. / Saboury, Ali Akbar et al. | 2019
- 310
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Targeting Loxosceles spider Sphingomyelinase D with small-molecule inhibitors as a potential therapeutic approach for loxoscelismLopes, Priscila Hess / Murakami, Mário T. / Portaro, Fernanda C. V. / Mesquita Pasqualoto, Kerly Fernanda / van den Berg, Carmen / Tambourgi, Denise V. et al. | 2019
- 322
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Synthesis and in vitro anticancer activity of certain novel 1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas as apoptosis-inducing agentsEldehna, Wagdy M. / Hassan, Ghada S. / Al-Rashood, Sara T. / Al-Warhi, Tarfah / Altyar, Ahmed E. / Alkahtani, Hamad M. / Almehizia, Abdulrahman A. / Abdel-Aziz, Hatem A. et al. | 2019
- 333
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Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitorsBrito, Camila C. Bitencourt / Silva, Hélder Vinicius Carneiro da / Brondani, Daci José / Faria, Antonio Rodolfo de / Ximenes, Rafael Matos / Silva, Ivanildo Mangueira da / Albuquerque, Julianna F. C. de / Castilho, Marcelo Santos et al. | 2019
- 343
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Synthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine moietiesPayaz, Deniz Üzeroğlu / Küçükbay, F. Zehra / Küçükbay, Hasan / Angeli, Andrea / Supuran, Claudiu T. et al. | 2019
- 350
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Soyasaponins from Zolfino bean as aldose reductase differential inhibitorsBalestri, Francesco / De Leo, Marinella / Sorce, Carlo / Cappiello, Mario / Quattrini, Luca / Moschini, Roberta / Pineschi, Carlotta / Braca, Alessandra / La Motta, Concettina / Da Settimo, Federico et al. | 2019
- 361
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The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1Xu, Xinyuan / Chen, Yingyi / Fu, Qiang / Ni, Duan / Zhang, Jian / Li, Xiaolong / Lu, Shaoyong et al. | 2019
- 375
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Synthesis and biological evaluation of novel N9-heterobivalent β-carbolines as angiogenesis inhibitorsGuo, Liang / Ma, Qin / Chen, Wei / Fan, Wenxi / Zhang, Jie / Dai, Bin et al. | 2019
- 388
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Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XIISeršen, Sara / Traven, Katja / Kljun, Jakob / Turel, Iztok / Supuran, Claudiu T. et al. | 2019
- 394
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A mitochondrial-targeted peptide ameliorated podocyte apoptosis through a HOCl-alb-enhanced and mitochondria-dependent signalling pathway in diabetic rats and in vitroWang, Xiaoqiao / Tang, Dongdong / Zou, Yaowei / Wu, Xiaoyu / Chen, Yihua / Li, Hongying / Chen, Siqi / Shi, Yue / Niu, Hongxin et al. | 2019
- 405
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Trypsin inhibitors: promising candidate satietogenic proteins as complementary treatment for obesity and metabolic disorders?Cristina Oliveira de Lima, Vanessa / Piuvezam, Grasiela / Leal Lima Maciel, Bruna / Heloneida de Araújo Morais, Ana et al. | 2019
- 420
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A feature-based analysis identifies COL1A2 as a regulator in pancreatic cancerWu, Jie / Liu, Jing / Wei, XiaoQing / Yu, Qi / Niu, XiangHuan / Tang, ShuHong / Song, Lei et al. | 2019
- 429
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Inhibition of acetylcholinesterase and butyrylcholinesterase with uracil derivatives: kinetic and computational studiesCavdar, Huseyin / Senturk, Murat / Guney, Murat / Durdagi, Serdar / Kayik, Gulru / Supuran, Claudiu T. / Ekinci, Deniz et al. | 2019
- 438
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Structure-guided design of anti-cancer ribonucleotide reductase inhibitorsMisko, Tessianna A. / Liu, Yi-Ting / Harris, Michael E. / Oleinick, Nancy L. / Pink, John / Lee, Hsueh-Yun / Dealwis, Chris G. et al. | 2019
- 451
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New sulfonamides containing organometallic-acylhydrazones: synthesis, characterisation and biological evaluation as inhibitors of human carbonic anhydrasesHuentupil, Yosselin / Peña, Luis / Novoa, Néstor / Berrino, Emanuela / Arancibia, Rodrigo / Supuran, Claudiu T. et al. | 2019
- 459
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Do CO2 and oxidative stress induce cancer?: a brief study about the evaluation of PON 1, CAT, CA and XO enzyme levels on head and neck cancer patientsMutlu, Murad / Korkmaz, M. Hakan / Simsek, Ender / Terzi, Emine / Oz Bedir, Beyza Ecem / Uysal, Tugba Kevser / Bayir, Omer / Saylam, Guleser / Guler, Ozen Ozensoy et al. | 2019
- 465
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(E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activityHuan, Le Cong / Phuong, Cao Viet / Truc, Le Cong / Thanh, Vo Nguyen / Pham-The, Hai / Huong, Le-Thi-Thu / Thuan, Nguyen Thi / Park, Eun Jae / Ji, A Young / Kang, Jong Soon et al. | 2019
- 479
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Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer’s disease therapyPachón-Angona, Irene / Refouvelet, Bernard / Andrýs, Rudolf / Martin, Helène / Luzet, Vincent / Iriepa, Isabel / Moraleda, Ignacio / Diez-Iriepa, Daniel / Oset-Gasque, María-Jesús / Marco-Contelles, José et al. | 2019
- 490
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An AGT-based protein-tag system for the labelling and surface immobilization of enzymes on E. coli outer membraneMerlo, Rosa / Del Prete, Sonia / Valenti, Anna / Mattossovich, Rosanna / Carginale, Vincenzo / Supuran, Claudiu T. / Capasso, Clemente / Perugino, Giuseppe et al. | 2019
- 500
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Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systemsKónya, Zoltán / Bécsi, Bálint / Kiss, Andrea / Horváth, Dániel / Raics, Mária / Kövér, Katalin E. / Lontay, Beáta / Erdődi, Ferenc et al. | 2019
- 510
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Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitorsRogato, Alessandra / Del Prete, Sonia / Nocentini, Alessio / Carginale, Vincenzo / Supuran, Claudiu T. / Capasso, Clemente et al. | 2019
- 519
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Chemical composition and enzyme inhibition of Phytolacca dioica L. seeds extractsDi Petrillo, Amalia / María González-Paramás, Ana / Rosa, Antonella / Ruggiero, Valeria / Boylan, Fabio / Kumar, Amit / Pintus, Francesca / Santos-Buelga, Celestino / Fais, Antonella / Era, Benedetta et al. | 2019
- 528
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Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzymeAkdemir, Atilla / Angeli, Andrea / Göktaş, Füsun / Eraslan Elma, Pınar / Karalı, Nilgün / Supuran, Claudiu T. et al. | 2019
- 532
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Novel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and caspase-3-mediated apoptosisMaher, Mai / Kassab, Asmaa E. / Zaher, Ashraf F. / Mahmoud, Zeinab et al. | 2019
- 547
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Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocketAllangba, Koffi N’Guessan Placide Gabin / Keita, Mélalie / Kre N’Guessan, Raymond / Megnassan, Eugene / Frecer, Vladimir / Miertus, Stanislav et al. | 2019
- 562
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Benzylamides and piperazinoarylamides of ibuprofen as fatty acid amide hydrolase inhibitorsDeplano, Alessandro / Cipriano, Mariateresa / Moraca, Federica / Novellino, Ettore / Catalanotti, Bruno / Fowler, Christopher J. / Onnis, Valentina et al. | 2019
- 577
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Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationshipProença, Carina / Freitas, Marisa / Ribeiro, Daniela / Tomé, Sara M. / Oliveira, Eduardo F. T. / Viegas, Matilde F. / Araújo, Alberto N. / Ramos, Maria J. / Silva, Artur M. S. / Fernandes, Pedro A. et al. | 2019
- 589
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Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitorsPoli, Giulio / Lapillo, Margherita / Jha, Vibhu / Mouawad, Nayla / Caligiuri, Isabella / Macchia, Marco / Minutolo, Filippo / Rizzolio, Flavio / Tuccinardi, Tiziano / Granchi, Carlotta et al. | 2019
- 597
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4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysisSecci, Daniela / Carradori, Simone / Petzer, Anél / Guglielmi, Paolo / D’Ascenzio, Melissa / Chimenti, Paola / Bagetta, Donatella / Alcaro, Stefano / Zengin, Gokhan / Petzer, Jacobus P. et al. | 2019
- 613
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Effect of cinnamamides on atopic dermatitis through regulation of IL-4 in CD4+ cellsChoi, Eun-Ju / Ryu, Young Bae / Tang, Yujiao / Kim, Bo Ram / Lee, Woo Song / Debnath, Trishna / Fan, Meiqi / Lee, Hyun-Su / Kim, Eun-Kyung et al. | 2019
- 620
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Design and synthesis of 4-piperazinyl quinoline derived urea/thioureas for anti-breast cancer activity by a hybrid pharmacophore approachViswas, Raja Solomon / Pundir, Sheetal / Lee, Hoyun et al. | 2019
- 631
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Discovery of novel dual-active 3-(4-(dimethylamino)phenyl)-7-aminoalcoxy-coumarin as potent and selective acetylcholinesterase inhibitor and antioxidantde Souza, Gabriela Alves / da Silva, Soraia John / Del Cistia, Catarina de Nigris / Pitasse-Santos, Paulo / Pires, Lucas de Oliveira / Passos, Yulli Moraes / Cordeiro, Yraima / Cardoso, Cristiane Martins / Castro, Rosane Nora / Sant’Anna, Carlos Mauricio R. et al. | 2019
- 638
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Development of a novel, high-affinity ssDNA trypsin inhibitorMalicki, Stanislaw / Ksiazek, Miroslaw / Majewski, Pawel / Pecak, Aleksandra / Mydel, Piotr / Grudnik, Przemyslaw / Dubin, Grzegorz et al. | 2019
- 644
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Inhibition of α-, β-, γ-, δ-, ζ- and η-class carbonic anhydrases from bacteria, fungi, algae, diatoms and protozoans with famotidineAngeli, Andrea / Pinteala, Mariana / Maier, Stelian S. / Del Prete, Sonia / Capasso, Clemente / Simionescu, Bogdan C. / Supuran, Claudiu T. et al. | 2019
- 651
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Synthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agentsYang, Jie / Zhang, Pingping / Hu, Yuheng / Liu, Teng / Sun, Jie / Wang, Xiaojing et al. | 2019
- 657
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Chemically stable inhibitors of 14-3-3 protein–protein interactions derived from BV02Iralde-Lorente, Leire / Cau, Ylenia / Clementi, Letizia / Franci, Lorenzo / Tassone, Giusy / Valensin, Daniela / Mori, Mattia / Angelucci, Adriano / Chiariello, Mario / Botta, Maurizio et al. | 2019
- 665
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Design, synthesis, and biological evaluation of novel derivatives of dithiodiglycolic acid prepared via oxidative coupling of thiolsBakulina, Olga / Bannykh, Anton / Jovanović, Mirna / Domračeva, Ilona / Podolski-Renić, Ana / Žalubovskis, Raivis / Pešić, Milica / Dar’in, Dmitry / Krasavin, Mikhail et al. | 2019
- 672
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Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivativesEl-Sayed, Nahed N. E. / Almaneai, Norah M. / Ben Bacha, Abir / Al-Obeed, Omar / Ahmad, Rehan / Abdulla, Maha / Alafeefy, Ahmed M. et al. | 2019
- 684
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In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenograftsAlameh, Ghina / Emptoz-Bonneton, Agnès / Rolland de Ravel, Marc / Matera, Eva L. / Mappus, Elisabeth / Balaguer, Patrick / Rocheblave, Luc / Lomberget, Thierry / Dumontet, Charles / Le Borgne, Marc et al. | 2019
- 692
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Aberrant regulation favours matriptase proteolysis in neoplastic B-cells that co-express HAI-2Chiu, Yi-Lin / Wu, Yi-Ying / Barndt, Robert B. / Yeo, Yee Hui / Lin, Yu-Wen / Sytwo, Hou-Ping / Liu, Huan-Cheng / Xu, Yuan / Jia, Bailing / Wang, Jehng-Kang et al. | 2019
- 703
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Evaluation of the anticancer potential of a sulphonamide carbonic anhydrase IX inhibitor on cervical cancer cellsKoyuncu, Ismail / Tülüce, Yasin / Slahaddin Qadir, Hewa / Durgun, Mustafa / Supuran, Claudiu T. et al. | 2019
- 712
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New flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic propertiesEstrada-Valencia, Martín / Herrera-Arozamena, Clara / Pérez, Concepción / Viña, Dolores / Morales-García, José A. / Pérez-Castillo, Ana / Ramos, Eva / Romero, Alejandro / Laurini, Erik / Pricl, Sabrina et al. | 2019
- 728
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Delivering bioactive cyclic peptides that target Hsp90 as prodrugsHuo, Yuantao / Buckton, Laura K. / Bennett, Jack L. / Smith, Eloise C. / Byrne, Frances L. / Hoehn, Kyle L. / Rahimi, Marwa N. / McAlpine, Shelli R. et al. | 2019
- 740
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Exploring the activity of polyamine analogues on polyamine and spermine oxidase: methoctramine, a potent and selective inhibitor of polyamine oxidaseDi Paolo, Maria Luisa / Cervelli, Manuela / Mariottini, Paolo / Leonetti, Alessia / Polticelli, Fabio / Rosini, Michela / Milelli, Andrea / Basagni, Filippo / Venerando, Rina / Agostinelli, Enzo et al. | 2019
- 753
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Inhibition potential of phenolic constituents from the aerial parts of Tetrastigma hemsleyanum against soluble epoxide hydrolase and nitric oxide synthaseWang, Cai Yi / Lee, Sunggun / Jang, Hyun-Jae / Su, Xiang Dong / Wang, Heng-Shan / Kim, Young Ho / Yang, Seo Young et al. | 2019
- 761
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Synthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agentsLuan, Tian / Jin, Chunmei / Jin, Chun-Mei / Gong, Guo-Hua / Quan, Zhe-Shan et al. | 2019
- 773
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Novel Re(I) tricarbonyl coordination compounds based on 2-pyridyl-1,2,3-triazole derivatives bearing a 4-amino-substituted benzenesulfonamide arm: synthesis, crystal structure, computational studies and inhibitory activity against carbonic anhydrase I, II, and IX isoforms†Aimene, Yassine / Eychenne, Romain / Mallet-Ladeira, Sonia / Saffon, Nathalie / Winum, Jean-Yves / Nocentini, Alessio / Supuran, Claudiu T. / Benoist, Eric / Seridi, Achour et al. | 2019
- 783
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Osteopontin – a biomarker of disease, but also of stage stratification of the functional myocardial contractile deficit by chronic ischaemic heart diseaseCoculescu, Bogdan-Ioan / Manole, Gheorghe / Dincă, Gabi Valeriu / Coculescu, Elena Claudia / Berteanu, Cristina / Stocheci, Cristina Mariana et al. | 2019
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The protective role of jervine against radiation-induced gastrointestinal toxicityYakan, Selvinaz / Aydin, Tuba / Gulmez, Canan / Ozden, Ozkan / Eren Erdogan, Kivilcim / Daglioglu, Yusuf Kenan / Andic, Fundagul / Atakisi, Onur / Cakir, Ahmet et al. | 2019
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CRISPR/Cas9-based liver-derived reporter cells for screening of mPGES-1 inhibitorsChen, Zhanfei / Cai, Xiaoling / Li, Man / Yan, LinLin / Wu, Luxi / Wang, Xiaoqian / Tang, Nanhong et al. | 2019
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Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hoppingZhang, Zhimin / Gu, Lili / Wang, Beibei / Huang, Wenhai / Zhang, Yanmin / Ma, Zhen / Zeng, Shenxin / Shen, Zhengrong et al. | 2019
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The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitorYu, Qian / Chen, Yu / Yang, Hui / Zhang, Hong-Li / Agama, Keli / Pommier, Yves / An, Lin-Kun et al. | 2019
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New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agentsChiarelli, Laurent R. / Mori, Matteo / Beretta, Giangiacomo / Gelain, Arianna / Pini, Elena / Sammartino, Josè Camilla / Stelitano, Giovanni / Barlocco, Daniela / Costantino, Luca / Lapillo, Margherita et al. | 2019
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Design, synthesis, and apoptosis-promoting effect evaluation of novel pyrazole with benzo[d]thiazole derivatives containing aminoguanidine unitsLiu, Da Chuan / Gao, Mei Jia / Huo, Qiang / Ma, Tao / Wang, Ying / Wu, Cheng Zhu et al. | 2019
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Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profileMghwary, Aml E.-S. / Gedawy, Ehab M. / Kamal, Aliaa M. / Abuel-Maaty, Suzan M. et al. | 2019
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Sesquiterpenoids and 2-(2-phenylethyl)chromones respectively acting as α-glucosidase and tyrosinase inhibitors from agarwood of an Aquilaria plantYang, Li / Yang, Yi-Ling / Dong, Wen-Hua / Li, Wei / Wang, Pei / Cao, Xue / Yuan, Jing-Zhe / Chen, Hui-Qin / Mei, Wen-Li / Dai, Hao-Fu et al. | 2019
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SAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogsShalaby, Raed / Petzer, Jacobus P. / Petzer, Anél / Ashraf, Usman M. / Atari, Ealla / Alasmari, Fawaz / Kumarasamy, Sivarajan / Sari, Youssef / Khalil, Ashraf et al. | 2019
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In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimersJanockova, Jana / Korabecny, Jan / Plsikova, Jana / Babkova, Katerina / Konkolova, Eva / Kucerova, Dana / Vargova, Jana / Koval, Jan / Jendzelovsky, Rastislav / Fedorocko, Peter et al. | 2019
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Antioxidant activity and antibacterial evaluation of new thiazolin-4-one derivatives as potential tryptophanyl-tRNA synthetase inhibitorsStana, Anca / Vodnar, Dan C. / Marc, Gabriel / Benedec, Daniela / Tiperciuc, Brînduşa / Tamaian, Radu / Oniga, Ovidiu et al. | 2019
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Design, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanomaQin, Feifei / Wang, Yali / Jiang, Xian / Wang, Yujia / Zhang, Nan / Wen, Xiang / Wang, Lian / Jiang, Qinglin / He, Gu et al. | 2019
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Evaluation of caffeine as inhibitor against collagenase, elastase and tyrosinase using in silico and in vitro approachEun Lee, Kyung / Bharadwaj, Shiv / Yadava, Umesh / Gu Kang, Sang et al. | 2019
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Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanismDan, Wen-Jia / Zhang, Qiang / Zhang, Fan / Wang, Wei-Wei / Gao, Jin-Ming et al. | 2019
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Thermostability enhancement of the α-carbonic anhydrase from Sulfurihydrogenibium yellowstonense by using the anchoring-and-self-labelling-protein-tag system (ASLtag)Del Prete, Sonia / Merlo, Rosa / Valenti, Anna / Mattossovich, Rosanna / Rossi, Mosè / Carginale, Vincenzo / Supuran, Claudiu T. / Perugino, Giuseppe / Capasso, Clemente et al. | 2019
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Design, synthesis, and anticancer evaluation of novel quinoline derivatives of ursolic acid with hydrazide, oxadiazole, and thiadiazole moieties as potent MEK inhibitorsJin, Xiao-Yan / Chen, Hao / Li, Dong-Dong / Li, A-Liang / Wang, Wen-Yan / Gu, Wen et al. | 2019
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Probing the role of an invariant active site His in family GH1 β-glycosidasesStrazzulli, Andrea / Perugino, Giuseppe / Mazzone, Marialuisa / Rossi, Mosè / Withers, Stephen G. / Moracci, Marco et al. | 2019
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Design, synthesis and biological activity evaluation of a new class of 2,4-thiazolidinedione compounds as insulin enhancersHuiying, Zou / Guangying, Chen / Shiyang, Zhou et al. | 2019
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Kinetic and computational molecular docking simulation study of novel kojic acid derivatives as anti-tyrosinase and antioxidant agentsChen, Yan-Mei / Li, Chen / Zhang, Wen-Jing / Shi, Yan / Wen, Zi-Jie / Chen, Qing-Xi / Wang, Qin et al. | 2019
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A novel anti-platelet aggregation target of chinensinaphthol methyl ether and neojusticin B obtained from Rostellularia procumbens (L.) NeesWu, Songtao / Yang, Yanfang / Liu, Bo / Xie, Zhoutao / Xiong, Weichen / Hao, Pengfei / Xiao, Wenping / Sun, Yuan / Ai, Zhongzhu / Wu, Hezhen et al. | 2019
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Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligasesHrast, Martina / Rožman, Kaja / Ogris, Iza / Škedelj, Veronika / Patin, Delphine / Sova, Matej / Barreteau, Hélène / Gobec, Stanislav / Grdadolnik, Simona Golič / Zega, Anamarija et al. | 2019
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Molecular modeling studies on the interactions of 7-methoxytacrine-4-pyridinealdoxime, 4-PA, 2-PAM, and obidoxime with VX-inhibited human acetylcholinesterase: a near attack conformation approachda Silva, Jorge Alberto Valle / Nepovimova, Eugenie / Ramalho, Teodorico Castro / Kuca, Kamil / Celmar Costa França, Tanos et al. | 2019
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Novel sulfonamide benzoquinazolinones as dual EGFR/HER2 inhibitors, apoptosis inducers and radiosensitizersSoliman, Aiten M. / Alqahtani, Ali S. / Ghorab, Mostafa M. et al. | 2019
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Impact of phytosterols on liver and distal colon metabolome in experimental murine colitis model: an explorative studyIaccarino, Nunzia / Amato, Jussara / Pagano, Bruno / Di Porzio, Anna / Micucci, Matteo / Bolelli, Luca / Aldini, Rita / Novellino, Ettore / Budriesi, Roberta / Randazzo, Antonio et al. | 2019
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Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studiesAmmazzalorso, Alessandra / Carradori, Simone / Angeli, Andrea / Akdemir, Atilla / De Filippis, Barbara / Fantacuzzi, Marialuigia / Giampietro, Letizia / Maccallini, Cristina / Amoroso, Rosa / Supuran, Claudiu T. et al. | 2019
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Structure-based design generated novel hydroxamic acid based preferential HDAC6 lead inhibitor with on-target cytotoxic activity against primary choroid plexus carcinomaKassab, Shaymaa E. / Mowafy, Samar / Alserw, Aya M. / Seliem, Joustin A. / El-Naggar, Shahenda M. / Omar, Nesreen N. / Awad, Mohamed M. et al. | 2019
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Stereoselective pharmacokinetic and pharmacodynamic analysis of a CNS-active sulphamoylphenyl carbamate derivativeBibi, David / Shusterman, Bella / Nocentini, Alessio / Supuran, Claudiu T. / Bialer, Meir et al. | 2019
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Synthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agentsHu, Yu-Heng / Yang, Jie / Zhang, Yun / Liu, Ke-Chun / Liu, Teng / Sun, Jie / Wang, Xiao-Jing et al. | 2019
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Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cellsdos Santos, Mariana Bastos / Bertholin Anselmo, Daiane / de Oliveira, Jéssica Gisleine / Jardim-Perassi, Bruna V. / Alves Monteiro, Diego / Silva, Gabriel / Gomes, Eleni / Lucia Fachin, Ana / Marins, Mozart / de Campos Zuccari, Débora Aparecida Pires et al. | 2019
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Leishmania infantum arginase: biochemical characterization and inhibition by naturally occurring phenolic substancesGarcia, Andreza R. / Oliveira, Danielle M. P. / Claudia F. Amaral, Ana / Jesus, Jéssica B. / Rennó Sodero, Ana Carolina / Souza, Alessandra M. T. / Supuran, Claudiu T. / Vermelho, Alane B. / Rodrigues, Igor A. / Pinheiro, Anderson S. et al. | 2019
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Design, synthesis, molecular modelling, and biological evaluation of novel substituted pyrimidine derivatives as potential anticancer agents for hepatocellular carcinomaAhmed, Naglaa Mohamed / Youns, Mahmoud / Soltan, Moustafa Khames / Said, Ahmed Mohammed et al. | 2019
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Design and synthesis of novel pyrazolo[4,3-d]pyrimidines as potential therapeutic agents for acute lung injuryWang, Bao Shi / Huang, Xin / Chen, Liu Zeng / Liu, Ming Ming / Shi, Jing Bo et al. | 2019
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Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysisDi Paolo, Veronica / Fulci, Chiara / Rotili, Dante / Sciarretta, Francesca / Lucidi, Alessia / Morozzo della Rocca, Blasco / De Luca, Anastasia / Rosato, Antonio / Quintieri, Luigi / Caccuri, Anna Maria et al. | 2019
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Discovery and antitumor evaluation of novel inhibitors of spermine oxidaseSun, Lidan / Yang, Jianlin / Qin, Yu / Wang, Yanlin / Wu, Hongyan / Zhou, You / Cao, Chunyu et al. | 2019
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Identification of novel indole derivatives acting as inhibitors of the Keap1–Nrf2 interactionCosimelli, Barbara / Greco, Giovanni / Laneri, Sonia / Novellino, Ettore / Sacchi, Antonia / Amendola, Giorgio / Cosconati, Sandro / Bortolozzi, Roberta / Viola, Giampietro et al. | 2019
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Identification of phenazine analogue as a novel scaffold for thioredoxin reductase I inhibitors against Hep G2 cancer cell linesLiao, Jianming / Wang, Linlin / Wu, Zhongxi / Wang, Zhixiang / Chen, Jun / Zhong, Yucheng / Jiang, Feng / Lu, Yuanyuan et al. | 2019
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Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovaniNocentini, Alessio / Osman, Sameh M. / Rodrigues, Igor A. / Cardoso, Veronica S. / Alasmary, Fatmah Ali S. / AlOthman, Zeid / Vermelho, Alane B. / Gratteri, Paola / Supuran, Claudiu T. et al. | 2019
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Synthesis and biological evaluation of novel 8-substituted quinoline-2-carboxamides as carbonic anhydrase inhibitorsThacker, Pavitra S. / Shaikh, Pirpasha / Angeli, Andrea / Arifuddin, Mohammed / Supuran, Claudiu T. et al. | 2019
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The first activation study of the β-carbonic anhydrases from the pathogenic bacteria Brucella suis and Francisella tularensis with amines and amino acidsAngeli, Andrea / Del Prete, Sonia / Pinteala, Mariana / Maier, Stelian S. / Donald, William A. / Simionescu, Bogdan C. / Capasso, Clemente / Supuran, Claudiu T. et al. | 2019
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Seeking new approach for therapeutic treatment of cholera disease via inhibition of bacterial carbonic anhydrases: experimental and theoretical studies for sixteen benzenesulfonamide derivativesGitto, Rosaria / De Luca, Laura / Mancuso, Francesca / Del Prete, Sonia / Vullo, Daniela / Supuran, Claudiu T. / Capasso, Clemente et al. | 2019
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Activation of human α-carbonic anhydrase isoforms I, II, IV and VII with bis-histamine schiff bases and bis-spinaceamine substituted derivativesAkocak, Suleyman / Lolak, Nabih / Bua, Silvia / Nocentini, Alessio / Supuran, Claudiu T. et al. | 2019
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Synthesis of a new series of 3-functionalised-1-phenyl-1,2,3-triazole sulfamoylbenzamides as carbonic anhydrase I, II, IV and IX inhibitorsSwain, Baijayantimala / Angeli, Andrea / Angapelly, Srinivas / Thacker, Pavitra S. / Singh, Priti / Supuran, Claudiu T. / Arifuddin, Mohammed et al. | 2019
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Synthesis, activity evaluation, and pro-apoptotic properties of novel 1,2,4-triazol-3-amine derivatives as potent anti-lung cancer agentsSun, Xian-yu / Zhong, Chun-yan / Qiu, Qing-qing / Li, Zhen-wang / Liu, Mei-yu / Wang, Xin / Jin, Cheng-hao et al. | 2019
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1D NMR WaterLOGSY as an efficient method for fragment-based lead discoveryRaingeval, Claire / Cala, Olivier / Brion, Béatrice / Le Borgne, Marc / Hubbard, Roderick Eliot / Krimm, Isabelle et al. | 2019
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Synthesis, antiasthmatic, and insecticidal/antifungal activities of allosamidinsHuang, Gangliang / Huang, Hualiang et al. | 2019
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Discovery of aminopyridine-containing spiro derivatives as EGFR mutations inhibitorsYe, Lianbao / Zhao, Tao / Du, Wenjun / Li, Anhu / Gao, Wei / Li, Jingrong / Wang, Ling / Chen, Weiqiang et al. | 2019
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In vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamideKassem, Asmaa F. / Moustafa, Gaber O. / Nossier, Eman S. / Khalaf, Hemat S. / Mounier, Marwa M. / Al-Yousef, Suliman A. / Mahmoud, Sabry Y. et al. | 2019
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Novel phthalimide based analogues: design, synthesis, biological evaluation, and molecular docking studiesOthman, Ismail M. M. / Gad-Elkareem, Mohamed A. M. / El-Naggar, Mohamed / Nossier, Eman S. / Amr, Abd El-Galil E. et al. | 2019
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Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1Herman, Bianka Edina / Kiss, Anita / Wölfling, János / Mernyák, Erzsébet / Szécsi, Mihály / Schneider, Gyula et al. | 2019
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Potential multifunctional agents with anti-hepatoma and anti-inflammation properties by inhibiting NF-кB activationSu, Chang-Ming / Hou, Gui-Ge / Wang, Chun-Hua / Zhang, Hong-Qin / Yang, Cheng / Liu, Mei / Hou, Yun et al. | 2019
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10H-1,9-diazaphenothiazine and its 10-derivatives: synthesis, characterisation and biological evaluation as potential anticancer agentsMorak-Młodawska, Beata / Pluta, Krystian / Latocha, Małgorzata / Jeleń, Małgorzata / Kuśmierz, Dariusz / Suwińska, Kinga / Shkurenko, Aleksander / Czuba, Zenon / Jurzak, Magdalena et al. | 2019
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Non-covalent immunoproteasome inhibitors induce cell cycle arrest in multiple myeloma MM.1R cellsEttari, Roberta / Pallio, Giovanni / Pizzino, Gabriele / Irrera, Natasha / Zappalà, Maria / Maiorana, Santina / Di Chio, Carla / Altavilla, Domenica / Squadrito, Francesco / Bitto, Alessandra et al. | 2019
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Computer-aided design and synthesis of 3-carbonyl-5-phenyl-1H-pyrazole as highly selective and potent BRAFV600E and CRAF inhibitorKim, Jinwoong / Choi, Byeongha / Im, Daseul / Jung, Hoyong / Moon, Hyungwoo / Aman, Waqar / Hah, Jung-Mi et al. | 2019
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Carbazole scaffolds in cancer therapy: a review from 2012 to 2018Issa, Samar / Prandina, Anthony / Bedel, Nicolas / Rongved, Pål / Yous, Saïd / Le Borgne, Marc / Bouaziz, Zouhair et al. | 2019
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Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibitionElmeligie, Salwa / Aboul-Magd, Asmaa M. / Lasheen, Deena S. / Ibrahim, Tamer M. / Abdelghany, Tamer M. / Khojah, Sohair M. / Abouzid, Khaled A. M. et al. | 2019
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Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activityHao, Xin / Qi, Gang / Ma, Hongxing / Zhu, Changjin / Han, Zhongfei et al. | 2019
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Discovery of new butyrylcholinesterase inhibitors via structure-based virtual screeningAtatreh, Noor / Al Rawashdah, Sara / Al Neyadi, Shaikha S. / Abuhamdah, Sawsan M. / Ghattas, Mohammad A. et al. | 2019
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Anticancer sulfonamide hybrids that inhibit bladder cancer cells growth and migration as tubulin polymerisation inhibitorsLiu, Jia / Liu, Chunlai / Zhang, Xiling / Yu, Liu / Gong, Xue / Wang, Ping et al. | 2019
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New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moietyUgwuja, D. I. / Okoro, U. C. / Soman, S. S. / Soni, R. / Okafor, S. N. / Ugwu, D. I. et al. | 2019
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Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffoldRotondi, Giulia / Guglielmi, Paolo / Carradori, Simone / Secci, Daniela / De Monte, Celeste / De Filippis, Barbara / Maccallini, Cristina / Amoroso, Rosa / Cirilli, Roberto / Akdemir, Atilla et al. | 2019
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Synthesis and enzyme-based evaluation of analogues L-tyrosine thiol carboxylic acid inhibitor of metallo-β-lactamase IMP-1Khalili Arjomandi, Omid / Kavoosi, Mahboubeh / Adibi, Hadi et al. | 2019
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Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitorsNam, Yunju / Hwang, Dongkeun / Kim, Namdoo / Seo, Hong-Seog / Selim, Khalid B. / Sim, Taebo et al. | 2019
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Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasiTeixeira, Bárbara Velame Ferreira / Teles, André Lacerda Braga / Silva, Suellen Gonçalves da / Brito, Camila Carane Bitencourt / Freitas, Humberto Fonseca de / Pires, Acássia Benjamim Leal / Froes, Thamires Quadros / Castilho, Marcelo Santos et al. | 2019
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Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C proteaseMaseko, Sibusiso / Padayachee, Eden / Maphumulo, Siyabonga / Govender, Thavendran / Sayed, Yasien / Maguire, Glenn / Lin, Johnson / Naicker, Tricia / Baijnath, Sooraj / Gerhardus, Kruger Hendrik et al. | 2019
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Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitorsAl-Sanea, Mohammad M. / Elkamhawy, Ahmed / Paik, Sora / Bua, Silvia / Ha Lee, So / Abdelgawad, Mohamed A. / Roh, Eun Joo / Eldehna, Wagdy M. / Supuran, Claudiu T. et al. | 2019
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Design, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activitySabatier, Laureano L. / Palestro, Pablo H. / Enrique, Andrea V. / Pastore, Valentina / Sbaraglini, María L. / Martín, Pedro / Gavernet, Luciana et al. | 2019
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A fast, miniaturised in-vitro assay developed for quantification of lipase enzyme activityMenden, Ariane / Hall, Davane / Paris, Daniel / Mathura, Venkatarian / Crawford, Fiona / Mullan, Michael / Crynen, Stefan / Ait-Ghezala, Ghania et al. | 2019
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Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activityKwon, Mincheol / Ko, Sung-Kyun / Jang, Mina / Kim, Gun-Hee / Ryoo, In-Ja / Son, Sangkeun / Ryu, Hyung Won / Oh, Sei-Ryang / Lee, Won-Kyu / Kim, Bo Yeon et al. | 2019
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Dual-target anti-Alzheimer’s disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activityMi, Zhisheng / Gan, Bing / Yu, Sihang / Guo, Jianan / Zhang, Changjun / Jiang, Xiaoying / Zhou, Tao / Su, Jing / Bai, Renren / Xie, Yuanyuan et al. | 2019
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Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivityLangella, Emma / Alterio, Vincenzo / D’Ambrosio, Katia / Cadoni, Roberta / Winum, Jean-Yves / Supuran, Claudiu T. / Monti, Simona Maria / De Simone, Giuseppina / Di Fiore, Anna et al. | 2019
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Exploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approachDe Simone, Giuseppina / Di Fiore, Anna / Truppo, Emanuela / Langella, Emma / Vullo, Daniela / Supuran, Claudiu T. / Monti, Simona Maria et al. | 2019
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Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activityGuglielmi, Paolo / Secci, Daniela / Petzer, Anél / Bagetta, Donatella / Chimenti, Paola / Rotondi, Giulia / Ferrante, Claudio / Recinella, Lucia / Leone, Sheila / Alcaro, Stefano et al. | 2019
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Exploring new structural features of the 4-[(3-methyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzenesulphonamide scaffold for the inhibition of human carbonic anhydrasesDistinto, Simona / Meleddu, Rita / Ortuso, Francesco / Cottiglia, Filippo / Deplano, Serenella / Sequeira, Lisa / Melis, Claudia / Fois, Benedetta / Angeli, Andrea / Capasso, Clemente et al. | 2019
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Design, synthesis, in vitro potent antiproliferative activity, and kinase inhibitory effects of new triarylpyrazole derivatives possessing different heterocycle terminal moietiesGamal El-Din, Mahmoud M. / El-Gamal, Mohammed I. / Abdel-Maksoud, Mohammed S. / Yoo, Kyung Ho / Oh, Chang-Hyun et al. | 2019
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Synthesis and biological evaluation of novel N-(piperazin-1-yl)alkyl-1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential MEK inhibitorsChen, Hao / Qiao, Chao / Miao, Ting-Ting / Li, A-Liang / Wang, Wen-Yan / Gu, Wen et al. | 2019
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Synthesis, computational studies, tyrosinase inhibitory kinetics and antimelanogenic activity of hydroxy substituted 2-[(4-acetylphenyl)amino]-2-oxoethyl derivativesRafiq, Muhammad / Nazir, Yasir / Ashraf, Zaman / Rafique, Hummera / Afzal, Samina / Mumtaz, Amara / Hassan, Mubashir / Ali, Anser / Afzal, Khurram / Yousuf, Muhammad Rizwan et al. | 2019
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Towards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact of hinge interaction, and accessibility of their bioactive conformation on VEGFR-2 activitiesJaballah, Maiy Y. / Serya, Rabah A. T. / Saad, Nasser / Khojah, Sohair M. / Ahmed, Marawan / Barakat, Khaled / Abouzid, Khaled A. M. et al. | 2019
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Design and application of oral colon administration systemCheng, Hao / Huang, Shiyu / Huang, Gangliang et al. | 2019
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Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonistsLao, Kejing / Xun, Guoliang / Gou, Xingchun / Xiang, Hua et al. | 2019
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Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsteroneKe, Shaoyong / Zhang, Zhigang / Liu, Manli / Fang, Wei / Huang, Daye / Wan, Zhongyi / Zhou, Ronghua / Wang, Kaimei / Shi, Liqiao et al. | 2019
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An overview of carbonic anhydrases and membrane channels of synoviocytes in inflamed jointsJi, Min Jeong / Hong, Jeong Hee et al. | 2019
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Competitive α-glucosidase inhibitors, dihydrobenzoxanthones, from the barks of Artocarpus elasticusJenis, Janar / Baiseitova, Aizhamal / Yoon, Sang Hwa / Park, Chanin / Kim, Jeong Yoon / Li, Zuo Peng / Lee, Keun Woo / Park, Ki Hun et al. | 2019
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Novel tyrosinase inhibitory peptide with free radical scavenging abilityShen, Zhiwei / Wang, Yujiao / Guo, Zhen / Tan, Tingyuan / Zhang, Yi et al. | 2019
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Exosomes in head and neck cancer. Updating and revisitingZorrilla, Samuel Rodríguez / García, Abel García / Carrión, Andrés Blanco / Vila, Pilar Gándara / Martín, Manuel Somoza / Torreira, Mercedes Gallas / Sayans, Mario Pérez et al. | 2019
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Activation of α-, β-, γ- δ-, ζ- and η- class of carbonic anhydrases with amines and amino acids: a reviewAkocak, Suleyman / Supuran, Claudiu T. et al. | 2019
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Anti-Helicobacter pylori activity of ethoxzolamideModak, Joyanta K. / Tikhomirova, Alexandra / Gorrell, Rebecca J. / Rahman, Mohammad M. / Kotsanas, Despina / Korman, Tony M. / Garcia-Bustos, Jose / Kwok, Terry / Ferrero, Richard L. / Supuran, Claudiu T. et al. | 2019
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Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitorZhang, Yaling / Chen, Li / Li, Xiabing / Gao, Li / Hao, Yunxia / Li, Baolin / Yan, Yaping et al. | 2019
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Synthesis and in vitro and in vivo anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivativesGuo, Wei-Yun / Chen, Liu-Zeng / Shen, Bang-Nian / Liu, Xin-Hua / Tai, Guang-Ping / Li, Qing-Shan / Gao, Li / Ruan, Ban-Feng et al. | 2019
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Extraction and derivatisation of active polysaccharidesLiu, Yang / Huang, Gangliang et al. | 2019
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