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Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer J. Med. Chem. (IF 6.205) Pub Date : 2021-01-18 Yonggang Meng; Bin Yu; He Huang; Youmei Peng; Ertong Li; Yongfang Yao; Chuanjun Song; Wenquan Yu; Kaikai Zhu; Kai Wang; Dongxu Yi; Jinfa Du; Junbiao Chang
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Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis J. Med. Chem. (IF 6.205) Pub Date : 2021-01-15 Brandon T. Milliken; Clinton Elfers; Oleg G. Chepurny; Kylie S. Chichura; Ian R. Sweet; Tito Borner; Matthew R. Hayes; Bart C. De Jonghe; George G. Holz; Christian L. Roth; Robert P. Doyle
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Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors: Optimization of Whole-Cell Anticryptococcal Activity and Insights into the Structural Origins of Cryptococcal Selectivity J. Med. Chem. (IF 6.205) Pub Date : 2021-01-14 Paul T. Marcyk; Emmanuelle V. LeBlanc; Douglas A. Kuntz; Alice Xue; Francisco Ortiz; Richard Trilles; Stephen Bengtson; Tristan M. G. Kenney; David S. Huang; Nicole Robbins; Noelle S. Williams; Damian J. Krysan; Gilbert G. Privé; Luke Whitesell; Leah E. Cowen; Lauren E. Brown
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Discovery of the First Druggable GPR52 Antagonist to Treat Huntington’s Disease J. Med. Chem. (IF 6.205) Pub Date : 2021-01-14 Hidetoshi Komatsu
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2021: A New Year and New Directions for the Journal of Medicinal Chemistry J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Craig W. Lindsley
I was thrilled beyond belief at being named the new Editor-in-Chief (EIC) of the Journal of Medicinal Chemistry (JMC)—I have looked up to Philip S. Portoghese (EIC of JMC for over 40 years!) since I was a graduate student, and to now have his former role may be the height of my professional career. The drug discovery community owes Phil a great deal for his stewardship of the Journal and in developing
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Development and Therapeutic Potential of NUAKs Inhibitors J. Med. Chem. (IF 6.205) Pub Date : 2020-12-24 Muhammad Faisal; Jae Ho Kim; Kyung Ho Yoo; Eun Joo Roh; Soon Sun Hong; So Ha Lee
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Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer’s Disease Multitarget Drug Discovery? J. Med. Chem. (IF 6.205) Pub Date : 2020-12-21 Angela De Simone; Vincenzo Tumiatti; Vincenza Andrisano; Andrea Milelli
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Recent Update on Targeting c-MYC G-Quadruplexes by Small Molecules for Anticancer Therapeutics J. Med. Chem. (IF 6.205) Pub Date : 2020-12-23 Ritapa Chaudhuri; Semantee Bhattacharya; Jyotirmayee Dash; Santanu Bhattacharya
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The Mycobactin Biosynthesis Pathway: A Prospective Therapeutic Target in the Battle against Tuberculosis J. Med. Chem. (IF 6.205) Pub Date : 2020-12-29 Mousumi Shyam; Deepak Shilkar; Harshita Verma; Abhimanyu Dev; Barij Nayan Sinha; Federico Brucoli; Sanjib Bhakta; Venkatesan Jayaprakash
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Strategies for Targeting the NLRP3 Inflammasome in the Clinical and Preclinical Space J. Med. Chem. (IF 6.205) Pub Date : 2020-12-22 Adam G. Schwaid; Kerrie B. Spencer
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Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development J. Med. Chem. (IF 6.205) Pub Date : 2020-12-30 Lu Hou; Jian Rong; Ahmed Haider; Daisuke Ogasawara; Cassis Varlow; Michael A. Schafroth; Linjing Mu; Jiefeng Gan; Hao Xu; Christopher J. Fowler; Ming-Rong Zhang; Neil Vasdev; Simon Ametamey; Benjamin F. Cravatt; Lu Wang; Steven H. Liang
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Spirocyclic Scaffolds in Medicinal Chemistry J. Med. Chem. (IF 6.205) Pub Date : 2020-12-31 Kerstin Hiesinger; Dmitry Dar’in; Ewgenij Proschak; Mikhail Krasavin
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Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Cheng-Peng Sun; Xin-Yue Zhang; Christophe Morisseau; Sung Hee Hwang; Zhan-Jun Zhang; Bruce D. Hammock; Xiao-Chi Ma
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Peptide–Drug Conjugates with Different Linkers for Cancer Therapy J. Med. Chem. (IF 6.205) Pub Date : 2020-12-31 Mona Alas; Azam Saghaeidehkordi; Kamaljit Kaur
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TLR2 Agonistic Small Molecules: Detailed Structure–Activity Relationship, Applications, and Future Prospects J. Med. Chem. (IF 6.205) Pub Date : 2020-12-21 Arshpreet Kaur; Deepender Kaushik; Sakshi Piplani; Surinder K. Mehta; Nikolai Petrovsky; Deepak B. Salunke
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Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Jan Skácel; Barbara S. Slusher; Takashi Tsukamoto
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Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases J. Med. Chem. (IF 6.205) Pub Date : 2020-12-23 Pengfei Wang; Qijie Gong; Jiabao Hu; Xiang Li; Xiaojin Zhang
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PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease J. Med. Chem. (IF 6.205) Pub Date : 2020-12-24 Ariamala Gopalsamy; Ann E. Aulabaugh; Amey Barakat; Kevin C. Beaumont; Shawn Cabral; Daniel P. Canterbury; Agustin Casimiro-Garcia; Jeanne S. Chang; Ming Z. Chen; Chulho Choi; Robert L. Dow; Olugbeminiyi O. Fadeyi; Xidong Feng; Scott P. France; Roger M. Howard; Jay M. Janz; Jayasankar Jasti; Reema Jasuja; Lyn H. Jones; Amanda King-Ahmad; Kelly M. Knee; Jeffrey T. Kohrt; Chris Limberakis; Spiros Liras;
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Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis J. Med. Chem. (IF 6.205) Pub Date : 2021-01-05 Steven E. Van der Plas; Hans Kelgtermans; Oscar Mammoliti; Christel Menet; Giovanni Tricarico; Ann De Blieck; Caroline Joannesse; Tom De Munck; Dominique Lambin; Marlon Cowart; Sebastien Dropsit; Sebastien L. X. Martina; Maarten Gees; Anne-Sophie Wesse; Katja Conrath; Martin Andrews
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When Macrocyclic Peptides Meet the Crystal Structure of a Melanocortin Receptor J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Paolo Grieco
This work reveals some key factors for the design of a novel generation of selective melanocortin ligands at the MC4 receptor.
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Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure† J. Med. Chem. (IF 6.205) Pub Date : 2020-11-14 Charlotte Martin; Luis E. Gimenez; Savannah Y. Williams; Yu Jing; Yiran Wu; Charlie Hollanders; Olivier Van der Poorten; Simon Gonzalez; Kevin Van holsbeeck; Santo Previti; Arthur Lamouroux; Suwen Zhao; Dirk Tourwé; Raymond C. Stevens; Roger D. Cone; Steven Ballet
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Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift J. Med. Chem. (IF 6.205) Pub Date : 2021-01-01 Shivaji A. Thorat; Yoonji Lee; Aeran Jung; Jihyae Ann; Songyeon Ahn; Jisoo Baek; Dongxu Zuo; Nayeon Do; Jin Ju Jeong; Peter M. Blumberg; Timothy E. Esch; Noe A. Turcios; Larry V. Pearce; Hee-Jin Ha; Young Dong Yoo; Sunhye Hong; Sun Choi; Jeewoo Lee
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From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis J. Med. Chem. (IF 6.205) Pub Date : 2020-12-31 Bei-Er Jiang; Xingwu Jiang; Qiansen Zhang; Qiuwen Liang; Zi-Liang Qiu; Xiang-Bai Sun; Jun-Jie Yang; Si Chen; Chunyang Yi; Xiaolei Chai; Mingyao Liu; Li-Fang Yu; Weiqiang Lu; Han-Kun Zhang
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Covalent Inhibition of Bacterial Urease by Bifunctional Catechol-Based Phosphonates and Phosphinates J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Aikaterini Pagoni; Agnieszka Grabowiecka; Wojciech Tabor; Artur Mucha; Stamatia Vassiliou; Łukasz Berlicki
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Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design J. Med. Chem. (IF 6.205) Pub Date : 2020-12-30 Justin D. Dietrich; Kenton L. Longenecker; Noel S. Wilson; Christian Goess; Sanjay C. Panchal; Steven L. Swann; Andrew M. Petros; Adrian D. Hobson; David Ihle; Danying Song; Paul Richardson; Kenneth M. Comess; Philip B. Cox; Amanda Dombrowski; Kathy Sarris; Diana L. Donnelly-Roberts; David B. Duignan; Arthur Gomtsyan; Paul Jung; A. Chris Krueger; Suzanne Mathieu; Andrea McClure; Vincent S. Stoll; Jill
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Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers J. Med. Chem. (IF 6.205) Pub Date : 2020-12-24 Masaki Watanabe; Michiko Fujihara; Tomoharu Motoyama; Mayu Kawasaki; Shoya Yamada; Yuta Takamura; Sohei Ito; Makoto Makishima; Shogo Nakano; Hiroki Kakuta
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2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F420)-Dependent Nitroreductase (Ddn) J. Med. Chem. (IF 6.205) Pub Date : 2020-12-21 Yanlin Jian; He Eun Forbes; Fabian Hulpia; Martijn D. P. Risseeuw; Guy Caljon; Hélène Munier-Lehmann; Helena I. M. Boshoff; Serge Van Calenbergh
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3,4-Dihydropyrimidin-2(1H)-ones as Antagonists of the Human A2B Adenosine Receptor: Optimization, Structure–Activity Relationship Studies, and Enantiospecific Recognition J. Med. Chem. (IF 6.205) Pub Date : 2020-12-29 María Majellaro; Willem Jespers; Abel Crespo; María J. Núñez; Silvia Novio; Jhonny Azuaje; Rubén Prieto-Díaz; Claudia Gioé; Belma Alispahic; José Brea; María I. Loza; Manuel Freire-Garabal; Carlota Garcia-Santiago; Carlos Rodríguez-García; Xerardo García-Mera; Olga Caamaño; Christian Fernandez-Masaguer; Javier F. Sardina; Angela Stefanachi; Abdelaziz El Maatougui; Ana Mallo-Abreu; Johan Åqvist; Hugo
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Structure–Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D J. Med. Chem. (IF 6.205) Pub Date : 2020-12-31 Elliot D. Mock; Ioli Kotsogianni; Wouter P. F. Driever; Carmen S. Fonseca; Jelle M. Vooijs; Hans den Dulk; Constant A. A. van Boeckel; Mario van der Stelt
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Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Harue Sasaki; Hiroyuki Masuno; Haru Kawasaki; Ayana Yoshihara; Nobutaka Numoto; Nobutoshi Ito; Hiroaki Ishida; Keiko Yamamoto; Naoya Hirata; Yasunari Kanda; Emiko Kawachi; Hiroyuki Kagechika; Aya Tanatani
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Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Chih-Wei Fu; Han-En Tsai; Wei-Sheng Chen; Tzu-Ting Chang; Chia-Ling Chen; Pei-Wen Hsiao; Wen-Shan Li
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Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Yang Liu; Hanying Ruan; Ying Li; Guoliang Sun; Xiao Liu; Wenhui He; Fengfeng Mao; Miaomiao He; Liwei Yan; Guocai Zhong; Huan Yan; Wenhui Li; Zhiyuan Zhang
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Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Rachel A. Rowlands; Qiuyan Chen; Renee A. Bouley; Larisa V. Avramova; John J. G. Tesmer; Andrew D. White
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Tuning the Biological Activity of RGD Peptides with Halotryptophans† J. Med. Chem. (IF 6.205) Pub Date : 2020-12-24 Isabell Kemker; David C. Schröder; Rebecca C. Feiner; Kristian M. Müller; Antoine Marion; Norbert Sewald
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Structure–Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor J. Med. Chem. (IF 6.205) Pub Date : 2020-12-22 Kien Trân; Alexandre Murza; Xavier Sainsily; Eugénie Delile; Pierre Couvineau; Jérôme Côté; David Coquerel; Maude Peloquin; Mannix Auger-Messier; Michel Bouvier; Olivier Lesur; Philippe Sarret; Éric Marsault
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Engineering of Orally Available, Ultralong-Acting Insulin Analogues: Discovery of OI338 and OI320 J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Thomas B. Kjeldsen; František Hubálek; Tina M. Tagmose; Lone Pridal; Hanne H. F. Refsgaard; Trine Porsgaard; Sanne Gram-Nielsen; Lars Hovgaard; Henrik Valore; Martin Münzel; Claudia U. Hjørringgaard; Claus Bekker Jeppesen; Valentina Manfè; Thomas Hoeg-Jensen; Svend Ludvigsen; Peter Kresten Nielsen; Inger Lautrup-Larsen; Carsten E. Stidsen; Erik M. Wulff; Patrick W. Garibay; János T. Kodra; Erica Nishimura;
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Novel Nonsecosteroidal Vitamin D Receptor Modulator Combined with Gemcitabine Enhances Pancreatic Cancer Therapy through Remodeling of the Tumor Microenvironment J. Med. Chem. (IF 6.205) Pub Date : 2020-12-31 Zisheng Kang; Cong Wang; Yu Tong; Yanyi Li; Yi Gao; Siyuan Hou; Meixi Hao; Xiaolin Han; Bin Wang; Qianqian Wang; Can Zhang
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Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195) J. Med. Chem. (IF 6.205) Pub Date : 2020-12-24 Hengmiao Cheng; Suvi T. M. Orr; Simon Bailey; Alexei Brooun; Ping Chen; Judith G. Deal; Yali L. Deng; Martin P. Edwards; Gary M. Gallego; Neil Grodsky; Buwen Huang; Mehran Jalaie; Stephen Kaiser; Robert S. Kania; Susan E. Kephart; Jennifer Lafontaine; Martha A. Ornelas; Mason Pairish; Simon Planken; Hong Shen; Scott Sutton; Luke Zehnder; Chau D. Almaden; Shubha Bagrodia; Matthew D. Falk; Hovhannes
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A Novel Triphenylphosphonium Carrier to Target Mitochondria without Uncoupling Oxidative Phosphorylation J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Chaitanya A. Kulkarni; Brian D. Fink; Bettine E. Gibbs; Pratik R. Chheda; Meng Wu; William I. Sivitz; Robert J. Kerns
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Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2 J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Chunjian Liu; James Lin; Charles Langevine; Daniel Smith; Jianqing Li; John S. Tokarski; Javed Khan; Max Ruzanov; Joann Strnad; Adriana Zupa-Fernandez; Lihong Cheng; Kathleen M. Gillooly; David Shuster; Yifan Zhang; Anil Thankappan; Kim W. McIntyre; Charu Chaudhry; Paul A. Elzinga; Manoj Chiney; Anjaneya Chimalakonda; Louis J. Lombardo; John E. Macor; Percy H. Carter; James R. Burke; David S. Weinstein
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Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors J. Med. Chem. (IF 6.205) Pub Date : 2020-12-22 Christine Brotherton-Pleiss; Peibin Yue; Yinsong Zhu; Kayo Nakamura; Weiliang Chen; Wenzhen Fu; Casie Kubota; Jasmine Chen; Felix Alonso-Valenteen; Simoun Mikhael; Lali Medina-Kauwe; Marcus A. Tius; Francisco Lopez-Tapia; James Turkson
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Improving Thermodynamic Stability and Anticoagulant Activity of a Thrombin Binding Aptamer by Incorporation of 8-trifluoromethyl-2′-deoxyguanosine J. Med. Chem. (IF 6.205) Pub Date : 2020-12-08 Hong-Liang Bao; Takumi Ishizuka; Atsushi Yamashita; Eiji Furukoji; Yujiro Asada; Yan Xu
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Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies J. Med. Chem. (IF 6.205) Pub Date : 2021-01-04 Candice Soares de Melo; Vinayak Singh; Alissa Myrick; Sandile B. Simelane; Dale Taylor; Christel Brunschwig; Nina Lawrence; Dirk Schnappinger; Curtis A. Engelhart; Anuradha Kumar; Tanya Parish; Qin Su; Timothy G. Myers; Helena I. M. Boshoff; Clifton E. Barry, III; Frederick A. Sirgel; Paul D. van Helden; Kirsteen I. Buchanan; Tracy Bayliss; Simon R. Green; Peter C. Ray; Paul G. Wyatt; Gregory S. Basarab;
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Synthesis, Tumor Specificity, and Photosensitizing Efficacy of Erlotinib-Conjugated Chlorins and Bacteriochlorins: Identification of a Highly Effective Candidate for Photodynamic Therapy of Cancer J. Med. Chem. (IF 6.205) Pub Date : 2021-01-05 Ravindra R. Cheruku; Joseph Cacaccio; Farukh A. Durrani; Walter A. Tabaczynski; Ramona Watson; Kevin Siters; Joseph R. Missert; Erin C. Tracy; Mykhaylo Dukh; Khurshid Guru; Richard C. Koya; Pawel Kalinski; Heinz Baumann; Ravindra K. Pandey
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Berberine Directly Targets the NEK7 Protein to Block the NEK7–NLRP3 Interaction and Exert Anti-inflammatory Activity J. Med. Chem. (IF 6.205) Pub Date : 2020-12-01 Qingxuan Zeng; Hongbin Deng; Yinghong Li; Tianyun Fan; Yang Liu; Sheng Tang; Wei Wei; Xiaojia Liu; Xixi Guo; Jiandong Jiang; Yanxiang Wang; Danqing Song
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Tenofovir-Amino Acid Conjugates Act as Polymerase Substrates—Implications for Avoiding Cellular Phosphorylation in the Discovery of Nucleotide Analogues J. Med. Chem. (IF 6.205) Pub Date : 2020-12-23 Weijie Gu; Sergio Martinez; Hoai Nguyen; Hongtao Xu; Piet Herdewijn; Steven De Jonghe; Kalyan Das
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Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan–Kynurenine Pathway J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Yu Yang; Timothy Borel; Francisco de Azambuja; David Johnson; Jacob P. Sorrentino; Chinedum Udokwu; Ian Davis; Aimin Liu; Ryan A. Altman
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Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice J. Med. Chem. (IF 6.205) Pub Date : 2020-12-28 Elisabet Viayna; Nicolas Coquelle; Monika Cieslikiewicz-Bouet; Pedro Cisternas; Carolina A. Oliva; Elena Sánchez-López; Miren Ettcheto; Manuela Bartolini; Angela De Simone; Mattia Ricchini; Marisa Rendina; Mégane Pons; Omidreza Firuzi; Belén Pérez; Luciano Saso; Vincenza Andrisano; Florian Nachon; Xavier Brazzolotto; Maria Luisa García; Antoni Camins; Israel Silman; Ludovic Jean; Nibaldo C. Inestrosa;
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1-Methyl-1H-pyrazole-5-carboxamide Derivatives Exhibit Unexpected Acute Mammalian Toxicity J. Med. Chem. (IF 6.205) Pub Date : 2020-12-22 Sarah Preston; Jose Garcia-Bustos; Liam G. Hall; Sheree D. Martin; Thuy G. Le; Abhijit Kundu; Atanu Ghoshal; Nghi H. Nguyen; Yaqing Jiao; Banfeng Ruan; Lian Xue; Fei Huang; Bill C. H. Chang; Sean L. McGee; Timothy N. C. Wells; Michael J. Palmer; Abdul Jabbar; Robin B. Gasser; Jonathan B. Baell
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Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors J. Med. Chem. (IF 6.205) Pub Date : 2021-01-05 Ehesan U. Sharif; Jaroslaw Kalisiak; Kenneth V. Lawson; Dillon H. Miles; Eric Newcomb; Erick A. Lindsey; Brandon R. Rosen; Laurent P. P. Debien; Ada Chen; Xiaoning Zhao; Stephen W. Young; Nigel P. Walker; Norbert Sträter; Emma R. Scaletti; Lixia Jin; Guifen Xu; Manmohan R. Leleti; Jay P. Powers
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Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343 J. Med. Chem. (IF 6.205) Pub Date : 2020-12-30 Kayo Yukawa-Takamatsu; Yifei Wang; Masaki Watanabe; Yuta Takamura; Michiko Fujihara; Mariko Nakamura-Nakayama; Shoya Yamada; Shota Kikuzawa; Makoto Makishima; Mayu Kawasaki; Sohei Ito; Shogo Nakano; Hiroki Kakuta
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Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis J. Med. Chem. (IF 6.205) Pub Date : 2020-12-17 Zhen Dai; Xiao-yi Chen; Lu-yan An; Cui-cui Li; Ni Zhao; Fan Yang; Song-tao You; Chen-zhi Hou; Kan Li; Cheng Jiang; Qi-dong You; Bin Di; Li-li Xu
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Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management J. Med. Chem. (IF 6.205) Pub Date : 2020-12-29 Youyi Peng; Qiang Zhang; William J. Welsh
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Correction to Structure–Activity Relationship of SPOP Inhibitors against Kidney Cancer J. Med. Chem. (IF 6.205) Pub Date : 2020-12-27 Ze Dong; Zhen Wang; Zhong-Qiang Guo; Shouzhe Gong; Tao Zhang; Jiang Liu; Cheng Luo; Hualiang Jiang; Cai-Guang Yang
Pages 4855 and 4856. In Figures 4 and 5, the two images should be switched. Page 4865. In right column, under Author Information, the affiliations for Cai-Guang Yang should be “State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, UCAS,
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Correction to “Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein” J. Med. Chem. (IF 6.205) Pub Date : 2020-12-23 Mingliang Wang; Jianfeng Lu; Mi Wang; Chao-Yie Yang; Shaomeng Wang
Page 7510. SHP2-D26. The stereochemistry of SHP2-D26 in the TOC graphic was incorrect, and the correct TOC graphic is shown below. Similarly, the incorrect stereochemistry also appeared in the naming of the following compounds in the experimental part and the SMILE file in the Supporting Information. The correct compound names are shown below. N1-(3-((3-amino-5-(4-amino-4-methylpiperidin-1-yl)pyra
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Imidazopyridine-Based 5-HT6 Receptor Neutral Antagonists: Impact of N1-Benzyl and N1-Phenylsulfonyl Fragments on Different Receptor Conformational States J. Med. Chem. (IF 6.205) Pub Date : 2021-01-13 David Vanda; Vittorio Canale; Severine Chaumont-Dubel; Rafał Kurczab; Grzegorz Satała; Paulina Koczurkiewicz-Adamczyk; Martyna Krawczyk; Wojciech Pietruś; Klaudia Blicharz; Elżbieta Pękala; Andrzej J. Bojarski; Piotr Popik; Philippe Marin; Miroslav Soural; Paweł Zajdel
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Structure–Activity Relationship and Biological Investigation of SR18292 (16), a Suppressor of Glucagon-Induced Glucose Production J. Med. Chem. (IF 6.205) Pub Date : 2021-01-12 Hua Lin; Kfir Sharabi; Li Lin; Claudia Ruiz; Di Zhu; Michael D. Cameron; Scott J. Novick; Patrick R. Griffin; Pere Puigserver; Theodore M. Kamenecka
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The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with pan-Hsp90 Inhibition J. Med. Chem. (IF 6.205) Pub Date : 2021-01-11 Sanket J. Mishra; Weiya Liu; Kristin Beebe; Monimoy Banerjee; Caitlin N. Kent; Vitumbiko Munthali; John Koren, III; John A Taylor, III; Leonard M. Neckers; Jeffrey Holzbeierlein; Brian S. J. Blagg
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Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure–Activity Relationship, and Anticancer Activities J. Med. Chem. (IF 6.205) Pub Date : 2021-01-10 Linling Gan; Zongjie Gan; Yanrong Dan; Yaowei Li; Peiming Zhang; Shanwen Chen; Zaijun Ye; Tao Pan; Chunmei Wan; Xuelian Hu; Yu Yu
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Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity J. Med. Chem. (IF 6.205) Pub Date : 2021-01-10 Elena Bechthold; Julian A. Schreiber; Kirstin Lehmkuhl; Bastian Frehland; Dirk Schepmann; Freddy A. Bernal; Constantin Daniliuc; Inés Álvarez; Cristina Val Garcia; Thomas J. Schmidt; Guiscard Seebohm; Bernhard Wünsch
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