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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer J. Med. Chem. (IF 6.054) Pub Date : 2020-04-06 Jay B. Fell; John P. Fischer; Brian R. Baer; James F. Blake; Karyn Bouhana; David M. Briere; Karin D. Brown; Laurence E. Burgess; Aaron C. Burns; Michael R. Burkard; Harrah Chiang; Mark J. Chicarelli; Adam W. Cook; John J. Gaudino; Jill Hallin; Lauren Hanson; Dylan P. Hartley; Erik J. Hicken; Gary P. Hingorani; Ronald J. Hinklin; Macedonio J. Mejia; Peter Olson; Jennifer N. Otten; Susan P. Rhodes;
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CN128: A New Orally Active Hydroxypyridinone Iron Chelator J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Wenteng Chen; Xin Yuan; Zhi Li; Zidong Lu; Sisi Kong; Huidi Jiang; Houbing Du; Xiuhong Pan; Manasi Nandi; Xiaole Kong; Kathryn Brown; Zudong Liu; Guolin Zhang; Robert C. Hider; Yongping Yu
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Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Stella Cascioferro; Barbara Parrino; Daniela Carbone; Domenico Schillaci; Elisa Giovannetti; Girolamo Cirrincione; Patrizia Diana
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Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Nicole Blaquiere; Elisia Villemure; Steven T. Staben
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Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Scott J. Hecker; K. Raja Reddy; Olga Lomovskaya; David C. Griffith; Debora Rubio-Aparicio; Kirk Nelson; Ruslan Tsivkovski; Dongxu Sun; Mojgan Sabet; Ziad Tarazi; Jonathan Parkinson; Maxim Totrov; Serge H. Boyer; Tomasz W. Glinka; Orville A. Pemberton; Yu Chen; Michael N. Dudley
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Design, Synthesis, and Conformation–Activity Study of Unnatural Bridged Bicyclic Depsipeptides as Highly Potent Hypoxia Inducible Factor-1 Inhibitors and Antitumor Agents J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Kota Koike; Masanobu Nagano; Masahiro Ebihara; Tasuku Hirayama; Mieko Tsuji; Hiroaki Suga; Hideko Nagasawa
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Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads J. Med. Chem. (IF 6.054) Pub Date : 2020-04-02 Gemma E. Mudd; Amy Brown; Liuhong Chen; Katerine van Rietschoten; Sophie Watcham; Daniel P. Teufel; Silvia Pavan; Rachid Lani; Philip Huxley; Gavin S. Bennett
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Machine Learning in Mass Spectrometry: A MALDI-TOF MS Approach to Phenotypic Antibacterial Screening J. Med. Chem. (IF 6.054) Pub Date : 2020-04-01 Luuk N. van Oosten; Christian D. Klein
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Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer J. Med. Chem. (IF 6.054) Pub Date : 2020-04-01 Fumiyuki Shirai; Anna Mizutani; Yoko Yashiroda; Takeshi Tsumura; Yuko Kano; Yukiko Muramatsu; Tsubasa Chikada; Hitomi Yuki; Hideaki Niwa; Shin Sato; Kenichi Washizuka; Yasuko Koda; Yui Mazaki; Myung-Kyu Jang; Haruka Yoshida; Akiko Nagamori; Masayuki Okue; Takashi Watanabe; Kouichi Kitamura; Eiki Shitara; Teruki Honma; Takashi Umehara; Mikako Shirouzu; Takehiro Fukami; Hiroyuki Seimiya; Minoru Yoshida;
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2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment J. Med. Chem. (IF 6.054) Pub Date : 2020-04-01 Seungbeom Lee; Dae Gyu Kim; Kyeojin Kim; Taewoo Kim; Semi Lim; Hyejin Kong; Sunghoon Kim; Young-Ger Suh
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Structurally Strained Half-Sandwich Iridium(III) Complexes As Highly Potent Anticancer Agents J. Med. Chem. (IF 6.054) Pub Date : 2020-04-01 Ana C. Carrasco; Vanessa Rodríguez-Fanjul; Abraha Habtemariam; Ana M. Pizarro
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6-Arylmethylidene Penicillin-Based Sulfone Inhibitors for Repurposing Antibiotic Efficiency in Priority Pathogens J. Med. Chem. (IF 6.054) Pub Date : 2020-03-31 Diana Rodríguez; María Maneiro; Juan C. Vázquez-Ucha; Alejandro Beceiro; Concepción González-Bello
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Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model J. Med. Chem. (IF 6.054) Pub Date : 2020-03-31 Jihui Zhao; Rongrong Cui; Lihao Wang; Yingjia Chen; Zunyun Fu; Xiaoyu Ding; Chen Cui; Tianbiao Yang; Xutong Li; Yuan Xu; Kaixian Chen; Xiaomin Luo; Hualiang Jiang; Mingyue Zheng
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pH-Dependent Grafting of Cancer Cells with Antigenic Epitopes Promotes Selective Antibody-Mediated Cytotoxicity J. Med. Chem. (IF 6.054) Pub Date : 2020-03-30 Janessa Wehr; Eden L. Sikorski; Elizabeth Bloch; Mary S. Feigman; Noel J. Ferraro; Trevor R. Baybutt; Adam E. Snook; Marcos M. Pires; Damien Thévenin
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LMP2 Inhibitors as a Potential Treatment for Alzheimer’s Disease J. Med. Chem. (IF 6.054) Pub Date : 2020-03-30 Deepak Bhattarai; Min Jae Lee; Ahruem Baek; In Jun Yeo; Zachary Miller; Yu Mi Baek; Sukyeong Lee; Dong-Eun Kim; Jin Tae Hong; Kyung Bo Kim
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Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising Antiproliferative Activity J. Med. Chem. (IF 6.054) Pub Date : 2020-03-30 Jose M. Arencibia; Nicoletta Brindani; Sebastian Franco-Ulloa; Michela Nigro; Jissy Akkarapattiakal Kuriappan; Giuliana Ottonello; Sine Mandrup Bertozzi; Maria Summa; Stefania Girotto; Rosalia Bertorelli; Andrea Armirotti; Marco De Vivo
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Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin J. Med. Chem. (IF 6.054) Pub Date : 2020-03-30 Venkatesh Mayandi; Qingxiao Xi; Eunice Tze Leng Goh; Siew Kwan Koh; Thomas Yong Jie Toh; Veluchamy Amutha Barathi; Mobashar Hussain Urf Turabe Fazil; Madhavi Latha Somaraju Chalasani; Jayasudha Varadarajan; Darren Shu Jeng Ting; Roger W. Beuerman; Lai Wah Chan; Rupesh Agrawal; Timothy Mark Sebastian Barkham; Lei Zhou; Navin Kumar Verma; Rajamani Lakshminarayanan
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(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido)propanoic Acid as a Novel PSMA Targeting Scaffold for Prostate Cancer Imaging J. Med. Chem. (IF 6.054) Pub Date : 2020-03-30 Xiaojiang Duan; Futao Liu; Hongmok Kwon; Youngjoo Byun; Il Minn; Xuekang Cai; Jingming Zhang; Martin G. Pomper; Zhi Yang; Zhen Xi; Xing Yang
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Validation and Characterization of Five Distinct Novel Inhibitors of Human Cytomegalovirus J. Med. Chem. (IF 6.054) Pub Date : 2020-03-27 Arun Kapoor; Ayan K. Ghosh; Michael Forman; Xin Hu; Wenjuan Ye; Noel Southall; Juan Marugan; Robert F. Keyes; Brian C. Smith; David J. Meyers; Marc Ferrer; Ravit Arav-Boger
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N-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition J. Med. Chem. (IF 6.054) Pub Date : 2020-03-26 Daniele Piomelli; Laura Scalvini; Yannick Fotio; Alessio Lodola; Gilberto Spadoni; Giorgio Tarzia; Marco Mor
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Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds J. Med. Chem. (IF 6.054) Pub Date : 2020-03-26 Irene G. Salado; Abhimanyu K. Singh; Carlos Moreno-Cinos; Guna Sakaine; Marco Siderius; Pieter Van der Veken; An Matheeussen; Tiffany van der Meer; Payman Sadek; Sheraz Gul; Louis Maes; Geert-Jan Sterk; Rob Leurs; David Brown; Koen Augustyns
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How We Think about Targeting RNA with Small Molecules J. Med. Chem. (IF 6.054) Pub Date : 2020-03-26 Matthew G. Costales; Jessica L. Childs-Disney; Hafeez S. Haniff; Matthew D. Disney
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Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors J. Med. Chem. (IF 6.054) Pub Date : 2020-03-26 Simona Di Martino; Piero Tardia; Vincenzo Cilibrasi; Samantha Caputo; Marco Mazzonna; Debora Russo; Ilaria Penna; Natalia Realini; Natasha Margaroli; Marco Migliore; Daniela Pizzirani; Giuliana Ottonello; Sine Mandrup Bertozzi; Andrea Armirotti; Duc Nguyen; Ying Sun; Ernesto R. Bongarzone; Peter Lansbury; Min Liu; Renato Skerlj; Rita Scarpelli
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Drug Distribution in Living Cells via Label-Free Molecular Fingerprint J. Med. Chem. (IF 6.054) Pub Date : 2020-03-25 Samir F. El-Mashtoly
A new application of stimulated Raman scattering (SRS) uses the benefit of a label-free molecular fingerprint to image the uptake and distribution of an alkyne-based drug in living cells. This method delivers information on cellular molecular composition and drug–cell interaction, showing the potential of SRS in drug development.
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Investigation of Inactive-State κ Opioid Receptor Homodimerization via Single-Molecule Microscopy Using New Antagonistic Fluorescent Probes J. Med. Chem. (IF 6.054) Pub Date : 2020-03-25 Antonios Drakopoulos; Zsombor Koszegi; Yann Lanoiselée; Harald Hübner; Peter Gmeiner; Davide Calebiro; Michael Decker
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TREK Channel Family Activator with a Well-Defined Structure–Activation Relationship for Pain and Neurogenic Inflammation J. Med. Chem. (IF 6.054) Pub Date : 2020-03-24 Yunguang Qiu; Lu Huang; Jie Fu; Chenxia Han; Jing Fang; Ping Liao; Zhuo Chen; Yiqing Mo; Peihua Sun; Daqing Liao; Linghui Yang; Jing Wang; Qiansen Zhang; Jin Liu; Feng Liu; Tingting Liu; Wei Huang; Huaiyu Yang; Ruotian Jiang
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Discovery and Development of Small-Molecule Inhibitors of Glycogen Synthase J. Med. Chem. (IF 6.054) Pub Date : 2020-03-23 Buyun Tang; Mykhaylo S. Frasinyuk; Vimbai M. Chikwana; Krishna K. Mahalingan; Cynthia A. Morgan; Dyann M. Segvich; Svitlana P. Bondarenko; Galyna P. Mrug; Przemyslaw Wyrebek; David S. Watt; Anna A. DePaoli-Roach; Peter J. Roach; Thomas D. Hurley
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Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor J. Med. Chem. (IF 6.054) Pub Date : 2020-03-20 Desirée Bartolini; Francesca De Franco; Pierangelo Torquato; Rita Marinelli; Bruno Cerra; Riccardo Ronchetti; Arne Schon; Francesca Fallarino; Antonella De Luca; Guido Bellezza; Ivana Ferri; Angelo Sidoni; William G. Walton; Samuel J. Pellock; Matthew R. Redinbo; Sridhar Mani; Roberto Pellicciari; Antimo Gioiello; Francesco Galli
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Automated De Novo Design in Medicinal Chemistry: Which Types of Chemistry Does a Generative Neural Network Learn? J. Med. Chem. (IF 6.054) Pub Date : 2020-03-20 Christoph Grebner; Hans Matter; Alleyn T. Plowright; Gerhard Hessler
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Structure–Activity Relationship of Antischistosomal Ozonide Carboxylic Acids J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Jianbo Wu; Xiaofang Wang; Francis C. K. Chiu; Cécile Häberli; David M. Shackleford; Eileen Ryan; Sriraghavan Kamaraj; Vivek J. Bulbule; Alexander I. Wallick; Yuxiang Dong; Karen L. White; Paul H. Davis; Susan A. Charman; Jennifer Keiser; Jonathan L. Vennerstrom
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Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Joshua D. Hansen; Matthew Correa; Mark A. Nagy; Matt Alexander; Veronique Plantevin; Virginia Grant; Brandon Whitefield; Dehua Huang; Timothy Kercher; Roy Harris; Rama Krishna Narla; Jim Leisten; Yang Tang; Mehran Moghaddam; Katalin Ebinger; Joseph Piccotti; Courtney G. Havens; Brian Cathers; James Carmichael; Thomas Daniel; Rupert Vessey; Lawrence G. Hamann; Katerina Leftheris; Derek Mendy; Frans
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CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success? J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Sarah Diab; Mingfeng Yu; Shudong Wang
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Structure–Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Elisabeth Rexen Ulven; Tezz Quon; Eugenia Sergeev; Natasja Barki; Matjaz Brvar; Brian D. Hudson; Palash Dutta; Anders Højgaard Hansen; Line Ø. Bielefeldt; Andrew B. Tobin; Christine J. McKenzie; Graeme Milligan; Trond Ulven
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Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Yu-Hui Jin; Meng-Chen Lu; Yan Wang; Wen-Xin Shan; Xuan-Yu Wang; Qi-Dong You; Zheng-Yu Jiang
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Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer’s Disease J. Med. Chem. (IF 6.054) Pub Date : 2020-03-19 Sònia Abás; Sergio Rodríguez-Arévalo; Andrea Bagán; Christian Griñán-Ferré; Foteini Vasilopoulou; Iria Brocos-Mosquera; Carolina Muguruza; Belén Pérez; Elies Molins; F. Javier Luque; Pilar Pérez-Lozano; Steven de Jonghe; Dirk Daelemans; Lieve Naesens; José Brea; M. Isabel Loza; Elena Hernández-Hernández; Jesús A. García-Sevilla; M. Julia García-Fuster; Milica Radan; Teodora Djikic; Katarina Nikolic;
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Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells J. Med. Chem. (IF 6.054) Pub Date : 2020-03-18 Jussara Amato; Giulia Miglietta; Rita Morigi; Nunzia Iaccarino; Alessandra Locatelli; Alberto Leoni; Ettore Novellino; Bruno Pagano; Giovanni Capranico; Antonio Randazzo
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Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells J. Med. Chem. (IF 6.054) Pub Date : 2020-03-18 Zhaoping Pan; Xiang Li; Yujia Wang; Qinglin Jiang; Li Jiang; Min Zhang; Nan Zhang; Fengbo Wu; Bo Liu; Gu He
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Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity J. Med. Chem. (IF 6.054) Pub Date : 2020-03-17 Marta Serafini; Enza Torre; Silvio Aprile; Erika Del Grosso; Alessandro Gesù; Alessia Griglio; Giorgia Colombo; Cristina Travelli; Salvatore Paiella; Annalisa Adamo; Elena Orecchini; Alice Coletti; Maria Teresa Pallotta; Stefano Ugel; Alberto Massarotti; Tracey Pirali; Silvia Fallarini
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Metabolic and Pharmaceutical Aspects of Fluorinated Compounds J. Med. Chem. (IF 6.054) Pub Date : 2020-03-17 Benjamin M. Johnson; Yue-Zhong Shu; Xiaoliang Zhuo; Nicholas A. Meanwell
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Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe J. Med. Chem. (IF 6.054) Pub Date : 2020-03-16 Sonia Kołt; Tomasz Janiszewski; Dion Kaiserman; Sylwia Modrzycka; Scott J. Snipas; Guy Salvesen; Marcin Dra̧g; Phillip I. Bird; Paulina Kasperkiewicz
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Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease J. Med. Chem. (IF 6.054) Pub Date : 2020-03-16 Kristi A. Leonard; Lisa A. Madge; Paul J. Krawczuk; Aihua Wang; Kevin D. Kreutter; Genesis M. Bacani; Wenying Chai; Russell C. Smith; Mark S. Tichenor; Michael C. Harris; Ravi Malaviya; Mark Seierstad; Marguerite E. Johnson; Jennifer D. Venable; Suzie Kim; Gavin C. Hirst; Ashok S. Mathur; Tadimeti S. Rao; James P. Edwards; Michele C. Rizzolio; Tatiana Koudriakova
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Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase J. Med. Chem. (IF 6.054) Pub Date : 2020-03-16 Yuta Tanaka; Osamu Kurasawa; Akihiro Yokota; Michael G. Klein; Koji Ono; Bunnai Saito; Shigemitsu Matsumoto; Masanori Okaniwa; Geza Ambrus-Aikelin; Daisuke Morishita; Satoshi Kitazawa; Noriko Uchiyama; Kazumasa Ogawa; Hiromichi Kimura; Shinichi Imamura
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Identification of Potent In Vivo Autotaxin Inhibitors that Bind to Both Hydrophobic Pockets and Channels in the Catalytic Domain J. Med. Chem. (IF 6.054) Pub Date : 2020-03-13 Mitsuyasu Kawaguchi; Takayoshi Okabe; Shinichi Okudaira; Kotaro Hama; Kuniyuki Kano; Hiroshi Nishimasu; Hidehiko Nakagawa; Ryuichiro Ishitani; Hirotatsu Kojima; Osamu Nureki; Junken Aoki; Tetsuo Nagano
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A Physiologically Based in Silico Tool to Assess the Risk of Drug-Related Crystalluria J. Med. Chem. (IF 6.054) Pub Date : 2020-03-13 Zhenhong Li; John Litchfield; David A. Tess; Anthony A. Carlo; Heather Eng; Christopher Keefer; Tristan S. Maurer
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Discovery and SARs of 5-Chloro-N4-phenyl-N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors with Potent Antitumor Activity J. Med. Chem. (IF 6.054) Pub Date : 2020-03-12 Yang Wang; Xing Chen; Yaoyao Yan; Xiaochen Zhu; Mingming Liu; Xinhua Liu
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Bifunctional Molecules beyond PROTACs J. Med. Chem. (IF 6.054) Pub Date : 2020-03-11 Stuart J. Conway
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Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders J. Med. Chem. (IF 6.054) Pub Date : 2020-03-10 Xiaozheng Dou; Dinesh Nath; Henry Shin; Elmar Nurmemmedov; Philip C. Bourne; Jian-Xing Ma; Adam S. Duerfeldt
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Discovery and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease J. Med. Chem. (IF 6.054) Pub Date : 2020-03-05 Justin R. Harrison; Sandipan Sarkar; Shahienaz Hampton; Jennifer Riley; Laste Stojanovski; Christer Sahlberg; Pia Appelqvist; Jessey Erath; Vinodhini Mathan; Ana Rodriguez; Marcel Kaiser; Dolores Gonzalez Pacanowska; Kevin D. Read; Nils Gunnar Johansson; Ian H. Gilbert
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Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-26 Ling Tong,Wenping Li,Michael Man-Chu Lo,Xiaolei Gao,Jenny Miu-Chen Wai,Michael Rudd,David Tellers,Aniket Joshi,Zhizhen Zeng,Patricia Miller,Cristian Salinas,Kerry Riffel,Hyking Haley,Mona Purcell,Marie Holahan,Liza Gantert,Jeffrey W Schubert,Kristen Jones,James Mulhearn,Melissa Egbertson,Zhaoyang Meng,Barbara Hanney,Robert Gomez,Scott T Harrison,Paul McQuade,Tjerk Bueters,Jason Uslaner,John Morrow
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Serendipitous Discovery of Leucine and Methionine Depletion Agents during the Search for Polyamine Transport Inhibitors. J. Med. Chem. (IF 6.054) Pub Date : 2020-03-02 Chelsea Massaro,Jenna Thomas,Houssine Ikhlef,Sharifa Dinara,Sara Cronk,Holly Moots,Otto Phanstiel
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Dual Binding to Orthosteric and Allosteric Sites Enhances the Anticancer Activity of a TRAP1-Targeting Drug. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-18 Sung Hu,Mariarosaria Ferraro,Ajesh P Thomas,Jeong Min Chung,Nam Gu Yoon,Ji-Hoon Seol,Sangpil Kim,Han-Ul Kim,Mi Young An,Haewon Ok,Hyun Suk Jung,Ja-Hyoung Ryu,Giorgio Colombo,Byoung Heon Kang
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Optimization of 4-Aminopiperidines as Inhibitors of Influenza A Viral Entry That Are Synergistic with Oseltamivir. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-18 Irina N Gaisina,Norton P Peet,Han Cheng,Ping Li,Ruikun Du,Qinghua Cui,Kevin Furlong,Balaji Manicassamy,Michael Caffrey,Gregory R J Thatcher,Lijun Rong
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2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-11 Sanjay Bhattarai,Jan Pippel,Emma Scaletti,Riham Idris,Marianne Freundlieb,Georg Rolshoven,Christian Renn,Sang-Yong Lee,Aliaa Abdelrahman,Herbert Zimmermann,Ali El-Tayeb,Christa E Müller,Norbert Sträter
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Structure-Activity Relationship Studies on Diversified Salicylamide Derivatives as Potent Inhibitors of Human Adenovirus Infection. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-11 Jimin Xu,Judith Berastegui-Cabrera,Haiying Chen,Jerónimo Pachón,Jia Zhou,Javier Sánchez-Céspedes
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Design, Synthesis, and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-18 Ya'nan Yu,Yuqiao Han,Fupo Zhang,Zhenmei Gao,Tong Zhu,Suzhen Dong,Mingliang Ma
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Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-17 Carley J S Heck,Herana Kamal Seneviratne,Namandjé N Bumpus
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Novel, Self-Assembling Dimeric Inhibitors of Human β Tryptase. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-14 Sarah F Giardina,Douglas S Werner,Maneesh Pingle,Philip B Feinberg,Kenneth W Foreman,Donald E Bergstrom,Lee D Arnold,Francis Barany
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Structural Effect on Adjuvanticity of Saponins. J. Med. Chem. (IF 6.054) Pub Date : 2020-02-26 Pengfei Wang,Xiong Ding,Hyunjung Kim,Suzanne M Michalek,Ping Zhang
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Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8 J. Med. Chem. (IF 6.054) Pub Date : 2020-02-25 Yuguang Zhao; Jingshan Ren; James Hillier; Weixian Lu; E. Yvonne Jones
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Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib J. Med. Chem. (IF 6.054) Pub Date : 2020-02-24 Greta Bagnolini; Domenico Milano; Marcella Manerba; Fabrizio Schipani; Jose Antonio Ortega; Dario Gioia; Federico Falchi; Andrea Balboni; Fulvia Farabegoli; Francesca De Franco; Janet Robertson; Roberto Pellicciari; Isabella Pallavicini; Sebastiano Peri; Saverio Minucci; Stefania Girotto; Giuseppina Di Stefano; Marinella Roberti; Andrea Cavalli
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