Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors (Unknown)
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In:
Journal of Medicinal Chemistry
;
62
, 3
;
1138-1166
;
2019
- Article (Journal) / Electronic Resource
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Title:Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors
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Additional title:J. Med. Chem.
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Contributors:Vögerl, Katharina ( author ) / Ong, Nghia ( author ) / Senger, Johanna ( author ) / Herp, Daniel ( author ) / Schmidtkunz, Karin ( author ) / Marek, Martin ( author ) / Müller, Martin ( author ) / Bartel, Karin ( author ) / Shaik, Tajith B. ( author ) / Porter, Nicholas J. ( author )
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Published in:Journal of Medicinal Chemistry ; 62, 3 ; 1138-1166
-
Publisher:
- New search for: American Chemical Society
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Publication date:2019-02-14
-
ISSN:
-
Coden:
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DOI:
-
Type of media:Article (Journal)
-
Type of material:Electronic Resource
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Language:Unknown
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Source:
Table of contents – Volume 62, Issue 3
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.
- 1077
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Drug Metabolism and Toxicology Special Issue Call for PapersGuengerich, F. Peter / Georg, Gunda I. / Wang, Shaomeng et al. | 2019
- 1078
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Cubanes in Medicinal ChemistryReekie, Tristan A. / Williams, Craig M. / Rendina, Louis M. / Kassiou, Michael et al. | 2019
- 1096
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Overview of the Development of Glutaminase Inhibitors: Achievements and Future DirectionsXu, Xi / Meng, Ying / Li, Lei / Xu, Pengfei / Wang, Jubo / Li, Zhiyu / Bian, Jinlei et al. | 2019
- 1116
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Virtual Chemical LibrariesWalters, W. Patrick et al. | 2019
- 1125
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Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2Wu, Xiaoqin / Xu, Gang / Li, Xiaobo / Xu, Weiren / Li, Qianjin / Liu, Wei / Kirby, Karen A. / Loh, Mignon L. / Li, Jun / Sarafianos, Stefan G. et al. | 2019
- 1138
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Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 InhibitorsVögerl, Katharina / Ong, Nghia / Senger, Johanna / Herp, Daniel / Schmidtkunz, Karin / Marek, Martin / Müller, Martin / Bartel, Karin / Shaik, Tajith B. / Porter, Nicholas J. et al. | 2019
- 1167
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Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt AgonistYukawa, Tomoya / Nara, Yoshi / Kono, Mitsunori / Sato, Ayumu / Oda, Tsuneo / Takagi, Terufumi / Sato, Takayuki / Banno, Yoshihiro / Taya, Naohiro / Imada, Takashi et al. | 2019
- 1180
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Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral LeishmaniasisThomas, Michael G. / De Rycker, Manu / Ajakane, Myriam / Albrecht, Sébastian / Álvarez-Pedraglio, Ana Isabel / Boesche, Markus / Brand, Stephen / Campbell, Lorna / Cantizani-Perez, Juan / Cleghorn, Laura A.T. et al. | 2019
- 1203
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Discovery and Development of N‑[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H3 Receptor Inverse Agonist with Robust Wake-Promoting ActivityNirogi, Ramakrishna / Shinde, Anil / Mohammed, Abdul Rasheed / Badange, Rajesh Kumar / Reballi, Veena / Bandyala, Thrinath Reddy / Saraf, Sangram Keshari / Bojja, Kumar / Manchineella, Sravanthi / Achanta, Pramod Kumar et al. | 2019
- 1218
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Conversion of Quinazoline Modulators from Inhibitors to Activators of β‑GlucocerebrosidaseZheng, Jianbin / Jeon, Sohee / Jiang, Weilan / Burbulla, Lena F. / Ysselstein, Daniel / Oevel, Kristine / Krainc, Dimitri / Silverman, Richard B. et al. | 2019
- 1231
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Design of Novel Inhibitors of Human Thymidine Phosphorylase: Synthesis, Enzyme Inhibition, in Vitro Toxicity, and Impact on Human Glioblastoma Cancerde Moura Sperotto, Nathalia D. / Deves Roth, Candida / Rodrigues-Junior, Valnês S. / Ev Neves, Christiano / Reisdorfer Paula, Fávero / da Silva Dadda, Adilio / Bergo, Pedro / Freitas de Freitas, Talita / Souza Macchi, Fernanda / Moura, Sidnei et al. | 2019
- 1246
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Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4‑Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5Graziani, Davide / Caligari, Silvia / Callegari, Elisa / De Toma, Carlo / Longhi, Matteo / Frigerio, Fabio / Dilernia, Roberto / Menegon, Sergio / Pinzi, Luca / Pirona, Lorenza et al. | 2019
- 1274
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Design, Synthesis, and Biological Evaluation of 6‑Substituted Thieno[3,2‑d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule InhibitorsRomagnoli, Romeo / Prencipe, Filippo / Oliva, Paola / Baraldi, Stefania / Baraldi, Pier Giovanni / Schiaffino Ortega, Santiago / Chayah, Mariem / Kimatrai Salvador, Maria / Lopez-Cara, Luisa Carlota / Brancale, Andrea et al. | 2019
- 1291
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Antiproliferative and Antimigratory Effects of a Novel YAP–TEAD Interaction Inhibitor Identified Using in Silico Molecular DockingSmith, Sarah A. / Sessions, Richard B. / Shoemark, Deborah K. / Williams, Christopher / Ebrahimighaei, Reza / McNeill, Madeleine C. / Crump, Matthew P. / McKay, Tristan R. / Harris, Gemma / Newby, Andrew C. et al. | 2019
- 1306
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Heterocyclic Diamidine DNA Ligands as HOXA9 Transcription Factor Inhibitors: Design, Molecular Evaluation, and Cellular Consequences in a HOXA9-Dependant Leukemia Cell ModelDepauw, Sabine / Lambert, Mélanie / Jambon, Samy / Paul, Ananya / Peixoto, Paul / Nhili, Raja / Marongiu, Laura / Figeac, Martin / Dassi, Christelle / Paul-Constant, Charles et al. | 2019
- 1330
-
Design, Synthesis, and Biological Evaluation of New 1‑(Aryl‑1H‑pyrrolyl)(phenyl)methyl‑1H‑imidazole Derivatives as Antiprotozoal AgentsSaccoliti, Francesco / Madia, Valentina Noemi / Tudino, Valeria / De Leo, Alessandro / Pescatori, Luca / Messore, Antonella / De Vita, Daniela / Scipione, Luigi / Brun, Reto / Kaiser, Marcel et al. | 2019
- 1348
-
5,6,7,8-Tetrahydro-1,6-naphthyridine Derivatives as Potent HIV-1-Integrase-Allosteric-Site InhibitorsPeese, Kevin M. / Allard, Christopher W. / Connolly, Timothy / Johnson, Barry L. / Li, Chen / Patel, Manoj / Sorensen, Margaret E. / Walker, Michael A. / Meanwell, Nicholas A. / McAuliffe, Brian et al. | 2019
- 1362
-
Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture HealingAbdelsamie, Ahmed S. / Herath, Steven / Biskupek, Yannik / Börger, Carsten / Siebenbürger, Lorenz / Salah, Mohamed / Scheuer, Claudia / Marchais-Oberwinkler, Sandrine / Frotscher, Martin / Pohlemann, Tim et al. | 2019
- 1373
-
Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid ChannelChai, Hao / Cheng, Xi / Zhou, Bin / Zhao, Lifen / Lin, Xianhua / Huang, Dongping / Lu, Weiqiang / Lv, Hao / Tang, Feng / Zhang, Qiansen et al. | 2019
- 1385
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Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ ProtectionGranberg, Kenneth L. / Yuan, Zhong-Qing / Lindmark, Bo / Edman, Karl / Kajanus, Johan / Hogner, Anders / Malmgren, Marcus / O’Mahony, Gavin / Nordqvist, Anneli / Lindberg, Jan et al. | 2019
- 1407
-
Structure–Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor AgonistsSensfuss, Ulrich / Kruse, Thomas / Skyggebjerg, Rikke Bjerring / Uldam, Henriette Kold / Vestergaard, Bill / Huus, Kasper / Vinther, Tine Nygaard / Reinau, Marika Ejby / Schéele, Susanne / Clausen, Trine Ryberg et al. | 2019
- 1420
-
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)Hu, Jiantao / Hu, Biao / Wang, Mingliang / Xu, Fuming / Miao, Bukeyan / Yang, Chao-Yie / Wang, Mi / Liu, Zhaomin / Hayes, Daniel F. / Chinnaswamy, Krishnapriya et al. | 2019
- 1443
-
Inhibition of Inositol Polyphosphate Kinases by Quercetin and Related Flavonoids: A Structure–Activity AnalysisGu, Chunfang / Stashko, Michael A. / Puhl-Rubio, Ana C. / Chakraborty, Molee / Chakraborty, Anutosh / Frye, Stephen V. / Pearce, Kenneth H. / Wang, Xiaodong / Shears, Stephen B. / Wang, Huanchen et al. | 2019
- 1455
-
Functional Selectivity Revealed by N‑Methylation Scanning of Human Urotensin II and Related PeptidesMerlino, Francesco / Billard, Étienne / Yousif, Ali M. / Di Maro, Salvatore / Brancaccio, Diego / Abate, Luigi / Carotenuto, Alfonso / Bellavita, Rosa / d’Emmanuele di Villa Bianca, Roberta / Santicioli, Paolo et al. | 2019
- 1468
-
Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3H)‑ones and in Vivo Studies on a Surgically Induced Rat Model of OsteoarthritisAtobe, Masakazu / Nagami, Takamichi / Muramatsu, Shuji / Ohno, Takeshi / Kitagawa, Masayuki / Suzuki, Hiroko / Ishiguro, Masashi / Watanabe, Atsushi / Kawanishi, Masashi et al. | 2019
- 1484
-
Identification of Dihydrofuro[3,4‑d]pyrimidine Derivatives as Novel HIV‑1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical PropertiesKang, Dongwei / Zhang, Heng / Wang, Zhao / Zhao, Tong / Ginex, Tiziana / Luque, Francisco Javier / Yang, Yang / Wu, Gaochan / Feng, Da / Wei, Fenju et al. | 2019
- 1502
-
Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba SeriesTosh, Dilip K. / Rao, Harsha / Bitant, Amelia / Salmaso, Veronica / Mannes, Philip / Lieberman, David I. / Vaughan, Kelli L. / Mattison, Julie A. / Rothwell, Amy C. / Auchampach, John A. et al. | 2019
- 1523
-
Discovery of (R)‑8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4‑b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3H)‑one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological MalignanciesWang, Hui-Ling / Andrews, Kristin L. / Booker, Shon K. / Canon, Jude / Cee, Victor J. / Chavez, Frank / Chen, Yuping / Eastwood, Heather / Guerrero, Nadia / Herberich, Brad et al. | 2019
- 1541
-
In Vitro and in Vivo Antitumor Effects of Plant-Derived Miliusanes and Their Induction of Cellular SenescenceXu, Xin-Ya / Tsang, Siu Wai / Guan, Yi-Fu / Liu, Kang-Lun / Pan, Wen-Hui / Lam, Chu Shing / Lee, Kwan Ming / Xia, Yi-Xuan / Xie, Wen-Jian / Wong, Wing Yan et al. | 2019
- 1562
-
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of ToxoplasmosisHopper, Allen T. / Brockman, Adam / Wise, Andy / Gould, Julie / Barks, Jennifer / Radke, Joshua B. / Sibley, L. David / Zou, Yongmao / Thomas, Stephen et al. | 2019
- 1577
-
Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer TherapyChen, Yong / Yuan, Xue / Zhang, Wanhua / Tang, Minghai / Zheng, Li / Wang, Fang / Yan, Wei / Yang, Shengyong / Wei, Yuquan / He, Jun et al. | 2019
- 1593
-
Tricyclic IndazolesA Novel Class of Selective Estrogen Receptor Degrader AntagonistsScott, James S. / Bailey, Andrew / Buttar, David / Carbajo, Rodrigo J. / Curwen, Jon / Davey, Paul R. J. / Davies, Robert D. M. / Degorce, Sébastien L. / Donald, Craig / Gangl, Eric et al. | 2019
- 1609
-
Metal-Binding Pharmacophore Library Yields the Discovery of a Glyoxalase 1 InhibitorPerez, Christian / Barkley-Levenson, Amanda M. / Dick, Benjamin L. / Glatt, Peter F. / Martinez, Yadira / Siegel, Dionicio / Momper, Jeremiah D. / Palmer, Abraham A. / Cohen, Seth M. et al. | 2019
- 1626
-
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i SubunitsXin, Bo-Tao / Huber, Eva M. / de Bruin, Gerjan / Heinemeyer, Wolfgang / Maurits, Elmer / Espinal, Christofer / Du, Yimeng / Janssens, Marissa / Weyburne, Emily S. / Kisselev, Alexei F. et al. | 2019
- 1643
-
Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12)Ogasawara, Daisuke / Ichu, Taka-Aki / Jing, Hui / Hulce, Jonathan J. / Reed, Alex / Ulanovskaya, Olesya A. / Cravatt, Benjamin F. et al. | 2019
- 1657
-
Antioxidant-Inspired Drug Discovery: Antitumor Metabolite Is Formed in Situ from a Hydroxycinnamic Acid Derivative upon Free-Radical ScavengingFási, Laura / Di Meo, Florent / Kuo, Ching-Ying / Stojkovic Buric, Sonja / Martins, Ana / Kúsz, Norbert / Béni, Zoltán / Dékány, Miklós / Balogh, György Tibor / Pesic, Milica et al. | 2019
- 1669
-
Synthesis and Evaluation of a QS-17/18-Based Vaccine AdjuvantWang, Pengfei / Škalamera, Đani / Sui, Xianwei / Zhang, Ping / Michalek, Suzanne M. et al. | 2019
- 1677
-
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ‑LyaseHu, Youtian / Wang, Lu / Han, Xu / Zhou, Yueyang / Zhang, Tonghui / Wang, Li / Hong, Ting / Zhang, Wei / Guo, Xun-Xiang / Sun, Jielin et al. | 2019
- 1684
-
Identification of the Metabolic Profile of the α‑Tubulin-Binding Natural Product (−)–PironetinCoulup, Sara K. / Huang, David S. / Wong, Henry L. / Georg, Gunda I. et al. | 2019
- 1690
-
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N‑(2-(1H‑1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)Reed, Carson W. / Yohn, Samantha E. / Washecheck, Jordan P. / Roenfanz, Hanna F. / Quitalig, Marc C. / Luscombe, Vincent B. / Jenkins, Matthew T. / Rodriguez, Alice L. / Engers, Darren W. / Blobaum, Anna L. et al. | 2019
- 1696
-
Correction to Targeting Myeloid Differentiation Using Potent 2‑Hydroxypyrazolo[1,5‑a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase InhibitorsSainas, Stefano / Pippione, Agnese C. / Lupino, Elisa / Giorgis, Marta / Circosta, Paola / Gaidano, Valentina / Goyal, Parveen / Bonanni, Davide / Rolando, Barbara / Cignetti, Alessandro et al. | 2019
- 1697
-
Correction to Targeting Tyrosinase: Development and Structural Insights of Novel Inhibitors Bearing Arylpiperidine and Arylpiperazine FragmentsFerro, Stefania / Deri, Batel / Germanò, Maria Paola / Gitto, Rosaria / Ielo, Laura / Buemi, Maria Rosa / Certo, Giovanna / Vittorio, Serena / Rapisarda, Antonio / Pazy, Yael et al. | 2019
- 1698
-
Correction to “Synthesis and Cytotoxic and Antiviral Profiling of Pyrrolo- and Furo-Fused 7‑Deazapurine Ribonucleosides”Tokarenko, Anna / Lišková, Barbora / Smoleń, Sabina / Táborská, Natálie / Tichý, Michal / Gurská, Soňa / Perlíková, Pavla / Frydrych, Ivo / Tloušt’ová, Eva / Znojek, Pawel et al. | 2019
- 1699
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Retraction of “CNS Physicochemical Property Space Shaped by a Diverse Set of Molecules with Experimentally Determined Exposure in the Mouse Brain”Rankovic, Zoran et al. | 2019