Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation (English)
- New search for: Zhang, Shao-Lin
- New search for: Zhang, Shao-Lin
- New search for: Hu, Xiaohui
- New search for: Zhang, Wen
- New search for: Tam, Kin Yip
In:
Journal of medicinal chemistry
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59
, 7
; 3562
;
2016
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ISSN:
- Article (Journal) / Print
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Title:Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation
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Contributors:
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Published in:Journal of medicinal chemistry ; 59, 7 ; 3562
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Publisher:
- New search for: American Chemical Society
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Place of publication:Easton, Pa.
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Publication date:2016
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 770/4230
- New search for: 44.42 / 44.42
- Further information on Basic classification
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Keywords:
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Source:
Table of contents – Volume 59, Issue 7
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.
- 2849
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Anti-HIV Drug Discovery and Development: Current Innovations and Future TrendsZhan, Peng / Pannecouque, Christophe / De Clercq, Erik / Liu, Xinyong et al. | 2016
- 2879
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Pharmacological Targeting of AMP-Activated Protein Kinase and Opportunities for Computer-Aided Drug DesignMiglianico, Marie / Nicolaes, Gerry A. F. / Neumann, Dietbert et al. | 2016
- 2894
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Small Molecule CXCR3 AntagonistsAndrews, Stephen P. / Cox, Rhona J. et al. | 2016
- 2918
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Discovery of a 9‑mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic PeptideHaug, Bengt Erik / Camilio, Ketil André / Eliassen, Liv Tone / Stensen, Wenche / Svendsen, John Sigurd / Berg, Kristel / Mortensen, Bjarte / Serin, Guillaume / Mirjolet, Jean-Francois / Bichat, Francis et al. | 2016
- 2928
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5‑((3-Amidobenzyl)oxy)nicotinamides as Sirtuin 2 InhibitorsAi, Teng / Wilson, Daniel J. / More, Swati S. / Xie, Jiashu / Chen, Liqiang et al. | 2016
- 2942
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Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6‑HydroxypyridazinonesCao, Xudong / Chen, Yin / Zhang, Yifang / Lan, Yu / Zhang, Juecheng / Xu, Xiangqing / Qiu, Yinli / Zhao, Song / Liu, Xin / Liu, Bi-Feng et al. | 2016
- 2962
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Discovery and Structure–Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac FunctionsMurza, Alexandre / Sainsily, Xavier / Coquerel, David / Côté, Jérôme / Marx, Patricia / Besserer-Offroy, Élie / Longpré, Jean-Michel / Lainé, Jean / Reversade, Bruno / Salvail, Dany et al. | 2016
- 2973
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Novel Analogues of (R)‑5-(Methylamino)-5,6-dihydro‑4H‑imidazo[4,5,1-ij]quinolin-2(1H)‑one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist SelectivityZou, Mu-Fa / Keck, Thomas M. / Kumar, Vivek / Donthamsetti, Prashant / Michino, Mayako / Burzynski, Caitlin / Schweppe, Catherine / Bonifazi, Alessandro / Free, R. Benjamin / Sibley, David R. et al. | 2016
- 2989
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Discovery of 5‑Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) LiabilitiesSakauchi, Nobuki / Kohara, Yasuhisa / Sato, Ayumu / Suzaki, Tomohiko / Imai, Yumi / Okabe, Yuichi / Imai, Shigemitsu / Saikawa, Reiko / Nagabukuro, Hiroshi / Kuno, Haruhiko et al. | 2016
- 3003
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Two New Faces of Amifostine: Protector from DNA Damage in Normal Cells and Inhibitor of DNA Repair in Cancer CellsHofer, Michal / Falk, Martin / Komůrková, Denisa / Falková, Iva / Bačíková, Alena / Klejdus, Bořivoj / Pagáčová, Eva / Štefančíková, Lenka / Weiterová, Lenka / Angelis, Karel J. et al. | 2016
- 3018
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Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1)Schmitt, Sven Marcel / Stefan, Katja / Wiese, Michael et al. | 2016
- 3034
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Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug DesignHan, Wooseok / Ding, Yu / Xu, Yongjin / Pfister, Keith / Zhu, Shejin / Warne, Bob / Doyle, Mike / Aikawa, Mina / Amiri, Payman / Appleton, Brent et al. | 2016
- 3046
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Design of Ionizable Lipids To Overcome the Limiting Step of Endosomal Escape: Application in the Intracellular Delivery of mRNA, DNA, and siRNAHabrant, Damien / Peuziat, Pauline / Colombani, Thibault / Dallet, Laurence / Gehin, Johan / Goudeau, Emilie / Evrard, Bérangère / Lambert, Olivier / Haudebourg, Thomas / Pitard, Bruno et al. | 2016
- 3063
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Structure–Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic CellsCherian, Joseph / Nacro, Kassoum / Poh, Zhi Ying / Guo, Samantha / Jeyaraj, Duraiswamy A. / Wong, Yun Xuan / Ho, Melvyn / Yang, Hai Yan / Joy, Joma Kanikadu / Kwek, Zekui Perlyn et al. | 2016
- 3079
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Tryptic Stability of Synthetic Bactenecin Derivatives Is Determined by the Side Chain Length of Cationic Residues and the Peptide ConformationBagheri, Mojtaba / Arasteh, Shima / Haney, Evan F. / Hancock, Robert E. W. et al. | 2016
- 3087
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The “Gatekeeper” Residue Influences the Mode of Binding of Acetyl Indoles to BromodomainsUnzue, Andrea / Zhao, Hongtao / Lolli, Graziano / Dong, Jing / Zhu, Jian / Zechner, Melanie / Dolbois, Aymeric / Caflisch, Amedeo / Nevado, Cristina et al. | 2016
- 3098
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A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel DiseaseKalindjian, S. Barret / Kadnur, Sanjay V. / Hewson, Christopher A. / Venkateshappa, Chandregowda / Juluri, Suresh / Kristam, Rajendra / Kulkarni, Bheemashankar / Mohammed, Zainuddin / Saxena, Rohit / Viswanadhan, Vellarkad N. et al. | 2016
- 3112
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An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor HomodimersLensing, Cody J. / Freeman, Katie T. / Schnell, Sathya M. / Adank, Danielle N. / Speth, Robert C. / Haskell-Luevano, Carrie et al. | 2016
- 3129
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Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide‑2 (GLP-2) Analogues with Low Systemic ClearanceWiśniewski, Kazimierz / Sueiras-Diaz, Javier / Jiang, Guangcheng / Galyean, Robert / Lu, Mark / Thompson, Dorain / Wang, Yung-Chih / Croston, Glenn / Posch, Alexander / Hargrove, Diane M. et al. | 2016
- 3140
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Antibacterial Diamines Targeting Bacterial MembranesWang, Bo / Pachaiyappan, Boobalan / Gruber, Jordon D. / Schmidt, Michael G. / Zhang, Yong-Mei / Woster, Patrick M. et al. | 2016
- 3152
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Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α‑Helical MimeticsWang, Ziqian / Song, Ting / Feng, Yingang / Guo, Zongwei / Fan, Yudan / Xu, Wenjie / Liu, Lu / Wang, Anhui / Zhang, Zhichao et al. | 2016
- 3163
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FimH Antagonists: Phosphate Prodrugs Improve Oral BioavailabilityKleeb, Simon / Jiang, Xiaohua / Frei, Priska / Sigl, Anja / Bezençon, Jacqueline / Bamberger, Karen / Schwardt, Oliver / Ernst, Beat et al. | 2016
- 3183
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Structure Property Relationships of Carboxylic Acid IsosteresLassalas, Pierrik / Gay, Bryant / Lasfargeas, Caroline / James, Michael J. / Tran, Van / Vijayendran, Krishna G. / Brunden, Kurt R. / Kozlowski, Marisa C. / Thomas, Craig J. / Smith, Amos B. et al. | 2016
- 3204
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Far-Red Light-Activatable Prodrug of Paclitaxel for the Combined Effects of Photodynamic Therapy and Site-Specific Paclitaxel ChemotherapyThapa, Pritam / Li, Mengjie / Bio, Moses / Rajaputra, Pallavi / Nkepang, Gregory / Sun, Yajing / Woo, Sukyung / You, Youngjae et al. | 2016
- 3215
-
Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) InfectionsWang, Youxin / Chen, Feifei / Di, Hongxia / Xu, Yong / Xiao, Qiang / Wang, Xuehai / Wei, Hanwen / Lu, Yanli / Zhang, Lingling / Zhu, Jin et al. | 2016
- 3231
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman PrimatesMandal, Mihirbaran / Wu, Yusheng / Misiaszek, Jeffrey / Li, Guoqing / Buevich, Alexei / Caldwell, John P. / Liu, Xiaoxiang / Mazzola, Robert D. / Orth, Peter / Strickland, Corey et al. | 2016
- 3249
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Purine (N)‑Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor AgonistsTosh, Dilip K. / Ciancetta, Antonella / Warnick, Eugene / O’Connor, Robert / Chen, Zhoumou / Gizewski, Elizabeth / Crane, Steven / Gao, Zhan-Guo / Auchampach, John A. / Salvemini, Daniela et al. | 2016
- 3264
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Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β AgonistZheng, Yajun / Zhuang, Linghang / Fan, Kristi Yi / Tice, Colin M. / Zhao, Wei / Dong, Chengguo / Lotesta, Stephen D. / Leftheris, Katerina / Lindblom, Peter R. / Liu, Zhijie et al. | 2016
- 3272
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Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 InhibitorsKavanagh, Madeline E. / Coyne, Anthony G. / McLean, Kirsty J. / James, Guy G. / Levy, Colin W. / Marino, Leonardo B. / de Carvalho, Luiz Pedro S. / Chan, Daniel S. H. / Hudson, Sean A. / Surade, Sachin et al. | 2016
- 3303
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Fast and Efficient Fragment-Based Lead Generation by Fully Automated Processing and Analysis of Ligand-Observed NMR Binding DataPeng, Chen / Frommlet, Alexandra / Perez, Manuel / Cobas, Carlos / Blechschmidt, Anke / Dominguez, Santiago / Lingel, Andreas et al. | 2016
- 3311
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Identification of a Human Toll-Like Receptor (TLR) 8‑Specific Agonist and a Functional Pan-TLR Inhibitor in 2‑AminoimidazolesBeesu, Mallesh / Caruso, Giuseppe / Salyer, Alex C. D. / Shukla, Nijunj M. / Khetani, Karishma K. / Smith, Luke J. / Fox, Lauren M. / Tanji, Hiromi / Ohto, Umeharu / Shimizu, Toshiyuki et al. | 2016
- 3331
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Purification-Free Method for Preparing Technetium-99m-Labeled Multivalent Probes for Enhanced in Vivo Imaging of Saturable SystemsMizuno, Yuki / Uehara, Tomoya / Hanaoka, Hirofumi / Endo, Yota / Jen, Chun-Wei / Arano, Yasushi et al. | 2016
- 3340
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Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated MetabolismCarosati, Emanuele / Cosimelli, Barbara / Ioan, Pierfranco / Severi, Elda / Katneni, Kasiram / Chiu, Francis C. K. / Saponara, Simona / Fusi, Fabio / Frosini, Maria / Matucci, Rosanna et al. | 2016
- 3353
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Design, Synthesis, and Biological Evaluation of Imidazo[1,5‑a]quinoline as Highly Potent Ligands of Central Benzodiazepine ReceptorsCappelli, Andrea / Anzini, Maurizio / Castriconi, Federica / Grisci, Giorgio / Paolino, Marco / Braile, Carlo / Valenti, Salvatore / Giuliani, Germano / Vomero, Salvatore / Di Capua, Angela et al. | 2016
- 3373
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Substituted Indazoles as Nav1.7 Blockers for the Treatment of PainFrost, Jennifer M. / DeGoey, David A. / Shi, Lei / Gum, Rebecca J. / Fricano, Meagan M. / Lundgaard, Greta L. / El-Kouhen, Odile F. / Hsieh, Gin C. / Neelands, Torben / Matulenko, Mark A. et al. | 2016
- 3392
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Discovery of Entrectinib: A New 3‑Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c‑ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitorMenichincheri, Maria / Ardini, Elena / Magnaghi, Paola / Avanzi, Nilla / Banfi, Patrizia / Bossi, Roberto / Buffa, Laura / Canevari, Giulia / Ceriani, Lucio / Colombo, Maristella et al. | 2016
- 3409
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Double Methotrexate-Modified Neuropeptide Y Analogues Express Increased Toxicity and Overcome Drug Resistance in Breast Cancer CellsBöhme, David / Krieghoff, Jan / Beck-Sickinger, Annette G. et al. | 2016
- 3418
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Detection of in Vitro Metabolite Formation of Leflunomide: A Fluorescence Dynamics and Electronic Structure StudySharma, Poornima / Gangopadhyay, Debraj / Mishra, Phool Chand / Mishra, Hirdyesh / Singh, Ranjan K. et al. | 2016
- 3427
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Routes of Synthesis of Carbapenems for Optimizing Both the Inactivation of l,d‑Transpeptidase LdtMt1 of Mycobacterium tuberculosis and the Stability toward Hydrolysis by β‑Lactamase BlaCIannazzo, Laura / Soroka, Daria / Triboulet, Sébastien / Fonvielle, Matthieu / Compain, Fabrice / Dubée, Vincent / Mainardi, Jean-Luc / Hugonnet, Jean-Emmanuel / Braud, Emmanuelle / Arthur, Michel et al. | 2016
- 3439
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Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl MoietyChaudhary, Vikas / Venghateri, Jubina B. / Dhaked, Hemendra P. S. / Bhoyar, Anil S. / Guchhait, Sankar K. / Panda, Dulal et al. | 2016
- 3452
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Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor AgonistsGeyer, Roland / Nordemann, Uwe / Strasser, Andrea / Wittmann, Hans-Joachim / Buschauer, Armin et al. | 2016
- 3471
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Development of Glucose Regulated Protein 94-Selective Inhibitors Based on the BnIm and Radamide ScaffoldCrowley, Vincent M. / Khandelwal, Anuj / Mishra, Sanket / Stothert, Andrew R. / Huard, Dustin J. E. / Zhao, Jinbo / Muth, Aaron / Duerfeldt, Adam S. / Kizziah, James L. / Lieberman, Raquel L. et al. | 2016
- 3489
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Identification and in Vivo Evaluation of Liver X Receptor β‑Selective Agonists for the Potential Treatment of Alzheimer’s DiseaseStachel, Shawn J. / Zerbinatti, Celina / Rudd, Michael T. / Cosden, Mali / Suon, Sokreine / Nanda, Kausik K. / Wessner, Keith / DiMuzio, Jillian / Maxwell, Jill / Wu, Zhenhua et al. | 2016
- 3499
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Characterizing the Epothilone Binding Site on β‑Tubulin by Photoaffinity Labeling: Identification of β‑Tubulin Peptides TARGSQQY and TSRGSQQY as Targets of an Epothilone Photoprobe for Polymerized TubulinRanade, Adwait R. / Higgins, LeeAnn / Markowski, Todd W. / Glaser, Nicole / Kashin, Dmitry / Bai, Ruoli / Hong, Kwon Ho / Hamel, Ernest / Höfle, Gerhard / Georg, Gunda I. et al. | 2016
- 3515
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Effect of α‑Methyl versus α‑Hydrogen Substitution on Brain Availability and Tumor Imaging Properties of Heptanoic [F-18]Fluoroalkyl Amino Acids for Positron Emission Tomography (PET)Bouhlel, Ahlem / Alyami, Wadha / Li, Aixiao / Yuan, Liya / Rich, Keith / McConathy, Jonathan et al. | 2016
- 3532
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2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective InhibitorsPatel, Leena / Chandrasekhar, Jayaraman / Evarts, Jerry / Haran, Aaron C. / Ip, Carmen / Kaplan, Joshua A. / Kim, Musong / Koditek, David / Lad, Latesh / Lepist, Eve-Irene et al. | 2016
- 3549
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Synthesis of α,β-Unsaturated Carbonyl-Based Compounds, Oxime and Oxime Ether Analogs as Potential Anticancer Agents for Overcoming Cancer Multidrug Resistance by Modulation of Efflux Pumps in Tumor CellsQin, Hua-Li / Leng, Jing / Zhang, Cheng-Pan / Jantan, Ibrahim / Amjad, Muhammad Wahab / Sher, Muhammad / Naeem-ul-Hassan, Muhammad / Hussain, Muhammad Ajaz / Bukhari, Syed Nasir Abbas et al. | 2016
- 3562
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Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer ProliferationZhang, Shao-Lin / Hu, Xiaohui / Zhang, Wen / Tam, Kin Yip et al. | 2016
- 3569
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Total Synthesis of Laspartomycin C and Characterization of Its Antibacterial Mechanism of ActionKleijn, Laurens H. J. / Oppedijk, Sabine F. / van Harten, Roel M. / Martin-Visscher, Leah A. / Kemmink, Johan / Breukink, Eefjan / Martin, Nathaniel I. et al. | 2016
- 3575
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Correction to Novel Peptide–Doxorubucin Conjugates for Targeting Breast Cancer Cells Including the Multidrug Resistant CellsSoudy, Rania / Chen, Christopher / Kaur, Kamaljit et al. | 2016
- 3576
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Correction to Investigation of (E)‑3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-RegulatorsDegorce, Sébastien L. / Bailey, Andrew / Callis, Rowena / De Savi, Chris / Ducray, Richard / Lamont, Gillian / MacFaul, Philip / Maudet, Mickael / Martin, Scott / Morgentin, Rémy et al. | 2016
- 3577
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Correction to Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure–Activity Relationships of Novel 1‑(Imidazo[1,2‑a]pyridin-6-yl)pyridin-2(1H)‑one DerivativesIgawa, Hideyuki / Takahashi, Masashi / Kakegawa, Keiko / Kina, Asato / Ikoma, Minoru / Aida, Jumpei / Yasuma, Tsuneo / Kawata, Yayoi / Ashina, Shuntaro / Yamamoto, Syunsuke et al. | 2016