当前分类:医药 当前期刊:Journal of Medicinal Chemistry 加入关注 导出

“Addition” and “Subtraction”: Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2017-02-24

Xin Chen, John Giraldes, Elizabeth R. Sprague, Subarna Shakya, Zhuoliang Chen, Yaping Wang, Carol Joud, Simon Mathieu, Christine Hiu-Tung Chen, Christopher Straub, Jose Duca, Kristen Hurov, Yanqiu Yuan, Wenlin Shao, B. Barry Touré 

Discovery of Novel Disruptor of Silencing Telomeric 1-Like (DOT1L) Inhibitors using a Target-Specific Scoring Function for the (S)-Adenosyl-l-methionine (SAM)-Dependent Methyltransferase Family 

J. Med. Chem. ( IF 5.589 ) 2017-02-21

Yulan Wang, Linjuan Li, Bidong Zhang, Jing Xing, Shijie Chen, Wei Wan, Yakai Song, Hao Jiang, Hualiang Jiang, Cheng Luo, Mingyue Zheng 

Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders 

J. Med. Chem. ( IF 5.589 ) 2017-02-21

Laurent Gomez, Mark Eben Massari, Troy Vickers, Graeme Freestone, William Vernier, Kiev Ly, Rui Xu, Margaret McCarrick, Tami Marrone, Markus Metz, Yingzhou G. Yan, Zachary W. Yoder, Robert Lemus, Nicola J. Broadbent, Richard Barido, Noelle Warren, Kara Schmelzer, David Neul, Dong Lee, Carsten B. Andersen, Kristen Sebring, Kathleen Aertgeerts, Xianbo Zhou, Ali Tabatabaei, Marco Peters, J. Guy Breitenbucher 

Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone–Naphthalimide–Polyamine Conjugates with Antimetastatic Activity 

J. Med. Chem. ( IF 5.589 ) 2017-02-21

Fujun Dai, Qian Li, Yuxia Wang, Chaochao Ge, Chenyang Feng, Songqiang Xie, Haoying He, Xiaojuan Xu, Chaojie Wang 

Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2017-02-20

Anna Vulpetti, Stefan Randl, Simon Rüdisser, Nils Ostermann, Paul Erbel, Aengus Mac Sweeney, Thomas Zoller, Bahaa Salem, Bernd Gerhartz, Frederic Cumin, Ulrich Hommel, Claudio Dalvit, Edwige Lorthiois, Jürgen Maibaum 

Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment 

J. Med. Chem. ( IF 5.589 ) 2017-02-17

Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti 

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans 

J. Med. Chem. ( IF 5.589 ) 2017-02-16

Atli Thorarensen, Martin E. Dowty, Mary Ellen Banker, Brian Juba, Jason Jussif, Tsung Lin, Fabien Vincent, Robert M. Czerwinski, Agustin Casimiro-Garcia, Ray Unwalla, John I. Trujillo, Sidney Liang, Paul Balbo, Ye Che, Adam M. Gilbert, Matthew F. Brown, Matthew Hayward, Justin Montgomery, Louis Leung, Xin Yang, Sarah Soucy, Martin Hegen, Jotham Coe, Jonathan Langille, Felix Vajdos, Jill Chrencik, Jean-Baptiste Telliez 

Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation 

J. Med. Chem. ( IF 5.589 ) 2017-02-16

Solomon Tadesse, Mingfeng Yu, Laychiluh B. Mekonnen, Frankie Lam, Saiful Islam, Khamis Tomusange, Muhammed H. Rahaman, Benjamin Noll, Sunita K. C. Basnet, Theodosia Teo, Hugo Albrecht, Robert Milne, Shudong Wang 

Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators 

J. Med. Chem. ( IF 5.589 ) 2017-02-16

Willem-Jan Keune, Frances Potjewyd, Tatjana Heidebrecht, Fernando Salgado-Polo, Simon J. F. Macdonald, Lakshman Chelvarajan, Ahmed Abdel Latif, Sony Soman, Andrew J. Morris, Allan J. B. Watson, Craig Jamieson, Anastassis Perrakis 

Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Paul A. Brough, Lisa Baker, Simon Bedford, Kirsten Brown, Seema Chavda, Victoria Chell, Jalanie D’Alessandro, Nicholas G. M. Davies, Ben Davis, Loic Le Strat, Alba T. Macias, Daniel Maddox, Patrick C. Mahon, Andrew J. Massey, Natalia Matassova, Sean McKenna, Jonathan D. Moore, James B. Murray, Christopher J. Northfield, Charles Parry, Rachel Parsons, Stephen D. Roughley, Terry Shaw, Heather Simmonite, Stephen Stokes, Allan Surgenor, Emma Stefaniak, Alan Robertson, Yikang Wang, Paul Webb, Neil Wh 

Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Sandeep Sundriyal, Sébastien Moniot, Zimam Mahmud, Shang Yao, Paolo Di Fruscia, Christopher R. Reynolds, David T. Dexter, Michael J. E. Sternberg, Eric W.-F. Lam, Clemens Steegborn, Matthew J. Fuchter 

Identification of High-Potency Human TLR8 and Dual TLR7/TLR8 Agonists in Pyrimidine-2,4-diamines 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Mallesh Beesu, Alex C. D. Salyer, Michael J. H. Brush, Kathryn L. Trautman, Justin K. Hill, Sunil A. David 

Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Sabin Llona-Minguez, Andreas Höglund, Elisee Wiita, Ingrid Almlöf, André Mateus, José Manuel Calderón-Montaño, Cindy Cazares-Körner, Evert Homan, Olga Loseva, Pawel Baranczewski, Ann-Sofie Jemth, Maria Häggblad, Ulf Martens, Bo Lundgren, Per Artursson, Thomas Lundbäck, Annika Jenmalm Jensen, Ulrika Warpman Berglund, Martin Scobie, Thomas Helleday 

Emergence of Small-Molecule Non-RGD-Mimetic Inhibitors for RGD Integrins 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Lisa M. Miller, John M. Pritchard, Simon J. F. Macdonald, Craig Jamieson, Allan J. B. Watson 

Transition State-Based Sialyltransferase Inhibitors: Mimicking Oxocarbenium Ion by Simple Amide 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Jian Guo, Wenming Li, Weiwei Xue, Xin-Shan Ye 

Bitopic Ligands and Metastable Binding Sites: Opportunities for G Protein-Coupled Receptor (GPCR) Medicinal Chemistry 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Philipp Fronik, Birgit I. Gaiser, Daniel Sejer Pedersen 

Binding and Proton Blockage by Amantadine Variants of the Influenza M2WT and M2S31N Explained 

J. Med. Chem. ( IF 5.589 ) 2017-02-15

Christina Tzitzoglaki, Anna Wright, Kathrin Freudenberger, Anja Hoffmann, Ian Tietjen, Ioannis Stylianakis, Felix Kolarov, David Fedida, Michaela Schmidtke, Günter Gauglitz, Timothy A. Cross, Antonios Kolocouris 

Full Sequence Amino Acid Scanning of θ-Defensin RTD-1 Yields a Potent Anthrax Lethal Factor Protease Inhibitor 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Yilong Li, Andrew Gould, Teshome Aboye, Tao Bi, Leonard Breindel, Alexander Shekhtman, Julio A. Camarero 

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Christopher R. Coxon, Elizabeth Anscombe, Suzannah J. Harnor, Mathew P. Martin, Benoit Carbain, Bernard T. Golding, Ian R. Hardcastle, Lisa K. Harlow, Svitlana Korolchuk, Christopher J. Matheson, David R. Newell, Martin E. M. Noble, Mangaleswaran Sivaprakasam, Susan J. Tudhope, David M. Turner, Lan Z. Wang, Stephen R. Wedge, Christopher Wong, Roger J. Griffin, Jane A. Endicott, Céline Cano 

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Yan Xiong, Fengling Li, Nicolas Babault, Aiping Dong, Hong Zeng, Hong Wu, Xin Chen, Cheryl H. Arrowsmith, Peter J. Brown, Jing Liu, Masoud Vedadi, Jian Jin 

Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Dustin Siegel, Hon C. Hui, Edward Doerffler, Michael O. Clarke, Kwon Chun, Lijun Zhang, Sean Neville, Ernest Carra, Willard Lew, Bruce Ross, Queenie Wang, Lydia Wolfe, Robert Jordan, Veronica Soloveva, John Knox, Jason Perry, Michel Perron, Kirsten M. Stray, Ona Barauskas, Joy Y. Feng, Yili Xu, Gary Lee, Arnold L. Rheingold, Adrian S. Ray, Roy Bannister, Robert Strickley, Swami Swaminathan, William A. Lee, Sina Bavari, Tomas Cihlar, Michael K. Lo, Travis K. Warren, Richard L. Mackman 

Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure–Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Marco Pieroni, Elisa Azzali, Nicoletta Basilico, Silvia Parapini, Michal Zolkiewski, Claudia Beato, Giannamaria Annunziato, Agostino Bruno, Federica Vacondio, Gabriele Costantino 

Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Xiaofei Liang, Fengchao Lv, Beilei Wang, Kailin Yu, Hong Wu, Ziping Qi, Zongru Jiang, Cheng Chen, Aoli Wang, Weili Miao, Wenchao Wang, Zhenquan Hu, Juan Liu, Xiaochuan Liu, Zheng Zhao, Li Wang, Shanchuan Zhang, Zi Ye, Chu Wang, Tao Ren, Yinsheng Wang, Qingsong Liu, Jing Liu 

4-Hydroxyphenylpyruvate Dioxygenase and Its Inhibition in Plants and Animals: Small Molecules as Herbicides and Agents for the Treatment of Human Inherited Diseases 

J. Med. Chem. ( IF 5.589 ) 2017-02-14

Annalisa Santucci, Giulia Bernardini, Daniela Braconi, Elena Petricci, Fabrizio Manetti 

Design, Synthesis, and Antimicrobial Evaluation of a Novel Bone-Targeting Bisphosphonate-Ciprofloxacin Conjugate for the Treatment of Osteomyelitis Biofilms 

J. Med. Chem. ( IF 5.589 ) 2017-02-13

Parish P. Sedghizadeh, Shuting Sun, Adam F. Junka, Eric Richard, Keivan Sadrerafi, Susan Mahabady, Neema Bakhshalian, Natalia Tjokro, Marzenna Bartoszewicz, Monika Oleksy, Patrycja Szymczyk, Mark W. Lundy, Jeffrey D. Neighbors, R. Graham G. Russell, Charles E. McKenna, Frank H. Ebetino 

Symmetrically Substituted Xanthone Amphiphiles Combat Gram-Positive Bacterial Resistance with Enhanced Membrane Selectivity 

J. Med. Chem. ( IF 5.589 ) 2017-02-13

Shuimu Lin, Jun-Jie Koh, Thet Tun Aung, Fanghui Lim, Jianguo Li, Hanxun Zou, Lin Wang, Rajamani Lakshminarayanan, Chandra Verma, Yingjun Wang, Donald T. H. Tan, Derong Cao, Roger W. Beuerman, Li Ren, Shouping Liu 

Discovery of an Inhibitor of the Proteasome Subunit Rpn11 

J. Med. Chem. ( IF 5.589 ) 2017-02-13

Christian Perez, Jing Li, Francesco Parlati, Matthieu Rouffet, Yuyong Ma, Andrew L. Mackinnon, Tsui-Fen Chou, Raymond J. Deshaies, Seth M. Cohen 

A Novel Potent Anticancer Compound Optimized from a Natural Oridonin Scaffold Induces Apoptosis and Cell Cycle Arrest through the Mitochondrial Pathway 

J. Med. Chem. ( IF 5.589 ) 2017-02-13

Shengtao Xu, Hong Yao, Shanshan Luo, Yun-Kai Zhang, Dong-Hua Yang, Dahong Li, Guangyu Wang, Mei Hu, Yangyi Qiu, Xiaoming Wu, Hequan Yao, Weijia Xie, Zhe-Sheng Chen, Jinyi Xu 

Design, Synthesis, and Evaluation of Isaindigotone Derivatives To Downregulate c-myc Transcription via Disrupting the Interaction of NM23-H2 with G-Quadruplex 

J. Med. Chem. ( IF 5.589 ) 2017-02-13

Chan Shan, Jin-Wu Yan, Yu-Qing Wang, Tong Che, Zhou-Li Huang, Ai-Chun Chen, Pei-Fen Yao, Jia-Heng Tan, Ding Li, Tian-Miao Ou, Lian-Quan Gu, Zhi-Shu Huang 

Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer’s Disease 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Frederik J. R. Rombouts, José-Ignacio Andrés, Manuela Ariza, José Manuel Alonso, Nigel Austin, Astrid Bottelbergs, Lu Chen, Vladimir Chupakhin, Erna Cleiren, Katleen Fierens, Alberto Fontana, Xavier Langlois, Joseph E. Leenaerts, Jonas Mariën, Carolina Martínez Lamenca, Rhys Salter, Mark E. Schmidt, Paula Te Riele, Cindy Wintmolders, Andrés A. Trabanco, Wei Zhang, Gregor Macdonald, Dieder Moechars 

Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Sabrina Tassini, Liang Sun, Kristina Lanko, Emmanuele Crespan, Emily Langron, Federico Falchi, Miroslava Kissova, Jorge I. Armijos-Rivera, Leen Delang, Carmen Mirabelli, Johan Neyts, Marco Pieroni, Andrea Cavalli, Gabriele Costantino, Giovanni Maga, Paola Vergani, Pieter Leyssen, Marco Radi 

Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Rui Xiong, Jiong Zhao, Lauren M. Gutgesell, Yueting Wang, Sue Lee, Bhargava Karumudi, Huiping Zhao, Yunlong Lu, Debra A. Tonetti, Gregory R. J. Thatcher 

Highly Potent Non-Carboxylic Acid Autotaxin Inhibitors Reduce Melanoma Metastasis and Chemotherapeutic Resistance of Breast Cancer Stem Cells 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Souvik Banerjee, Derek D. Norman, Sue Chin Lee, Abby L. Parrill, Truc Chi T. Pham, Daniel L. Baker, Gabor J. Tigyi, Duane D. Miller 

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhib 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Carolin Schwehm, Barrie Kellam, Aimie E. Garces, Stephen J. Hill, Nicholas D. Kindon, Tracey D. Bradshaw, Jin Li, Simon J. F. Macdonald, James E. Rowedder, Leigh A. Stoddart, Michael J. Stocks 

Design, Palladium-Catalyzed Synthesis, and Biological Investigation of 2-Substituted 3-Aroylquinolin-4(1H)-ones as Inhibitors of the Hedgehog Signaling Pathway 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Romina Alfonsi, Bruno Botta, Sandro Cacchi, Lucia Di Marcotullio, Giancarlo Fabrizi, Roberta Faedda, Antonella Goggiamani, Antonia Iazzetti, Mattia Mori 

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Philip A. Harris, Scott B. Berger, Jae U. Jeong, Rakesh Nagilla, Deepak Bandyopadhyay, Nino Campobasso, Carol A. Capriotti, Julie A. Cox, Lauren Dare, Xiaoyang Dong, Patrick M. Eidam, Joshua N. Finger, Sandra J. Hoffman, James Kang, Viera Kasparcova, Bryan W. King, Ruth Lehr, Yunfeng Lan, Lara K. Leister, John D. Lich, Thomas T. MacDonald, Nathan A. Miller, Michael T. Ouellette, Christina S. Pao, Attiq Rahman, Michael A. Reilly, Alan R. Rendina, Elizabeth J. Rivera, Michelle C. Schaeffer, Clark  

Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R) 

J. Med. Chem. ( IF 5.589 ) 2017-02-10

Vivek Kumar, Amy E. Moritz, Thomas M. Keck, Alessandro Bonifazi, Michael P. Ellenberger, Christopher D. Sibley, R. Benjamin Free, Lei Shi, J. Robert Lane, David R. Sibley, Amy Hauck Newman 

Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion 

J. Med. Chem. ( IF 5.589 ) 2017-02-09

Francisco José Fueyo González, Godwin U. Ebiloma, Carolina Izquierdo García, Victor Bruggeman, José María Sánchez Villamañán, Anne Donachie, Emmanuel Oluwadare Balogun, Daniel Ken Inaoka, Tomoo Shiba, Shigeharu Harada, Kiyoshi Kita, Harry P. de Koning, Christophe Dardonville 

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode 

J. Med. Chem. ( IF 5.589 ) 2017-02-09

Elizabeth A. Jurica, Ximao Wu, Kristin N. Williams, Andres S. Hernandez, David S. Nirschl, Richard A. Rampulla, Arvind Mathur, Min Zhou, Gary Cao, Chunshan Xie, Biji Jacob, Hong Cai, Tao Wang, Brian J. Murphy, Heng Liu, Carrie Xu, Lori K. Kunselman, Michael B. Hicks, Qin Sun, Dora M. Schnur, Doree F. Sitkoff, Elizabeth A. Dierks, Atsu Apedo, Douglas B. Moore, Kimberly A. Foster, Mary Ellen Cvijic, Reshma Panemangalore, Neil A. Flynn, Brad D. Maxwell, Yang Hong, Yuan Tian, Jason J. Wilkes, Bradle 

Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2017-02-08

Andrea Astolfi, Tommaso Felicetti, Nunzio Iraci, Giuseppe Manfroni, Serena Massari, Donatella Pietrella, Oriana Tabarrini, Glenn W. Kaatz, Maria L. Barreca, Stefano Sabatini, Violetta Cecchetti 

The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization 

J. Med. Chem. ( IF 5.589 ) 2017-02-08

Lewis D. Pennington, Demetri T. Moustakas 

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model 

J. Med. Chem. ( IF 5.589 ) 2017-02-07

Kawaljit Singh, John Okombo, Christel Brunschwig, Ferdinand Ndubi, Linley Barnard, Chad Wilkinson, Peter M. Njogu, Mathew Njoroge, Lizahn Laing, Marta Machado, Miguel Prudêncio, Janette Reader, Mariette Botha, Sindisiwe Nondaba, Lyn-Marie Birkholtz, Sonja Lauterbach, Alisje Churchyard, Theresa L. Coetzer, Jeremy N. Burrows, Clive Yeates, Paolo Denti, Lubbe Wiesner, Timothy J. Egan, Sergio Wittlin, Kelly Chibale 

Inhibitors of Influenza Virus Polymerase Acidic (PA) Endonuclease: Contemporary Developments and Perspectives 

J. Med. Chem. ( IF 5.589 ) 2017-02-07

Han Ju, Jian Zhang, Boshi Huang, Dongwei Kang, Bing Huang, Xinyong Liu, Peng Zhan 

Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856 

J. Med. Chem. ( IF 5.589 ) 2017-02-07

Stephane Perreault, Jayaraman Chandrasekhar, Zhi-Hua Cui, Jerry Evarts, Jia Hao, Joshua A. Kaplan, Adam Kashishian, Kathleen S. Keegan, Thomas Kenney, David Koditek, Latesh Lad, Eve-Irene Lepist, Mary E. McGrath, Leena Patel, Bart Phillips, Joseph Therrien, Jennifer Treiberg, Anella Yahiaoui, Gary Phillips 

Selective Inhibitors of Human Liver Carboxylesterase Based on a β-Lapachone Scaffold: Novel Reagents for Reaction Profiling 

J. Med. Chem. ( IF 5.589 ) 2017-02-07

M. Jason Hatfield, Jingwen Chen, Ellie M. Fratt, Liying Chi, John C. Bollinger, Randall J. Binder, John Bowling, Janice L. Hyatt, Jerrod Scarborough, Cynthia Jeffries, Philip M. Potter 

Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy 

J. Med. Chem. ( IF 5.589 ) 2017-02-06

Ying Huang, Jeff Zhang, Zhengtian Yu, Hailong Zhang, Youzhen Wang, Andreas Lingel, Wei Qi, Justin Gu, Kehao Zhao, Michael D. Shultz, Long Wang, Xingnian Fu, Yongfeng Sun, Qiong Zhang, Xiangqing Jiang, Jiangwei Zhang, Chunye Zhang, Ling Li, Jue Zeng, Lijian Feng, Chao Zhang, Yueqin Liu, Man Zhang, Lijun Zhang, Mengxi Zhao, Zhenting Gao, Xianghui Liu, Douglas Fang, Haibing Guo, Yuan Mi, Tobias Gabriel, Michael P. Dillon, Peter Atadja, Counde Oyang 

Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277 

J. Med. Chem. ( IF 5.589 ) 2017-02-06

Hanna Cho, Sandip Sengupta, Sean S. H. Jeon, Wooyoung Hur, Hwan Geun Choi, Hong-Seog Seo, Byung Joo Lee, Jeong Hun Kim, Minhwan Chung, Noo Li Jeon, Nam Doo Kim, Taebo Sim 

Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis 

J. Med. Chem. ( IF 5.589 ) 2017-02-03

Subramanyam J. Tantry, Shankar D. Markad, Vikas Shinde, Jyothi Bhat, Gayathri Balakrishnan, Amit K. Gupta, Anisha Ambady, Anandkumar Raichurkar, Chaitanyakumar Kedari, Sreevalli Sharma, Naina V. Mudugal, Ashwini Narayan, C. N. Naveen Kumar, Robert Nanduri, Sowmya Bharath, Jitendar Reddy, Vijender Panduga, K. R. Prabhakar, Karthikeyan Kandaswamy, Ramanatha Saralaya, Parvinder Kaur, Neela Dinesh, Supreeth Guptha, Kirsty Rich, David Murray, Helen Plant, Marian Preston, Helen Ashton, Darren Plant, J 

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Co 

J. Med. Chem. ( IF 5.589 ) 2017-02-03

Kellie D. Nance, Emily L. Days, C. David Weaver, Anastasia Coldren, Tiffany D. Farmer, Hyekyung P. Cho, Colleen M. Niswender, Anna L. Blobaum, Kevin D. Niswender, Craig W. Lindsley 

In Vitro and in Vivo Evaluation of Fully Substituted (5-(3-Ethoxy-3-oxopropynyl)-4-(ethoxycarbonyl)-1,2,3-triazolyl-glycosides as Original Nucleoside Analogues to Circumvent Resistance in Myeloid Malignancies 

J. Med. Chem. ( IF 5.589 ) 2017-02-02

Hella Amdouni, Guillaume Robert, Mohsine Driowya, Nathan Furstoss, Camille Métier, Alix Dubois, Maeva Dufies, Marwa Zerhouni, François Orange, Sandra Lacas-Gervais, Khalid Bougrin, Anthony R. Martin, Patrick Auberger, Rachid Benhida 

Nanomolar-Potency Aminophenyl-1,3,5-triazine Activators of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Chloride Channel for Prosecretory Therapy of Dry Eye Diseases 

J. Med. Chem. ( IF 5.589 ) 2017-01-31

Sujin Lee, Puay-Wah Phuan, Christian M. Felix, Joseph-Anthony Tan, Marc H. Levin, Alan S. Verkman 

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker 

J. Med. Chem. ( IF 5.589 ) 2017-01-31

James R. Corte, Tianan Fang, Honey Osuna, Donald J. P. Pinto, Karen A. Rossi, Joseph E. Myers, Steven Sheriff, Zhen Lou, Joanna J. Zheng, Timothy W. Harper, Jeffrey M. Bozarth, Yiming Wu, Joseph M. Luettgen, Dietmar A. Seiffert, Carl P. Decicco, Ruth R. Wexler, Mimi L. Quan 

Development of Dihydroxyphenyl Sulfonylisoindoline Derivatives as Liver-Targeting Pyruvate Dehydrogenase Kinase Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2017-01-31

Shih-Chia Tso, Mingliang Lou, Cheng-Yang Wu, Wen-Jun Gui, Jacinta L. Chuang, Lorraine K. Morlock, Noelle S. Williams, R. Max Wynn, Xiangbing Qi, David T. Chuang 

Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A 

J. Med. Chem. ( IF 5.589 ) 2017-01-31

Victoria A. Steadman, Simon B. Pettit, Karine G. Poullennec, Linos Lazarides, Andrew J. Keats, David K. Dean, Steven J. Stanway, Carol A. Austin, Jonathan A. Sanvoisin, Gregory M. Watt, Hans G. Fliri, Albert C. Liclican, Debi Jin, Melanie H. Wong, Stephanie A. Leavitt, Yu-Jen Lee, Yang Tian, Christian R. Frey, Todd C. Appleby, Uli Schmitz, Petr Jansa, Richard L. Mackman, Brian E. Schultz 

Design, Synthesis, and Biological Evaluation of Novel, Non-Brain-Penetrant, Hybrid Cannabinoid CB1R Inverse Agonist/Inducible Nitric Oxide Synthase (iNOS) Inhibitors for the Treatment of Liver Fibrosis 

J. Med. Chem. ( IF 5.589 ) 2017-01-27

Malliga R. Iyer, Resat Cinar, Alexis Katz, Michael Gao, Katalin Erdelyi, Tony Jourdan, Nathan J. Coffey, Pal Pacher, George Kunos 

Some contents have been Reproduced with permission of the American Chemical Society.
Some contents have been Reproduced by permission of The Royal Society of Chemistry.
所有期刊列表A-Z


【问答】有机机理考考你(十四)
简历润色
期刊订阅
化合物查询
试剂库存管理
down
wechat
bug