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Tranylcypromine based LSD1 inhibitor: Summary and Prospective. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-15 Xingjie Dai,Ying Liu,Xiaopeng Xiong,Leipeng Xue,Yi-Chao Zheng,Hongmin Liu
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Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Christian Gampe,Vishal A Verma
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Myeloid Differentiation Primary Response Protein 88 (MyD88): the central hub of TLR/IL-1R signaling. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-15 Lingfeng Chen,Lulu Zheng,Pengqin Chen,Guang Liang
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Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-10 James S Scott,Thomas A Moss,Amber Balazs,Bernard Barlaam,Jason Breed,Rodrigo Carbajo,Elisabetta Chiarparin,Paul Davey,Oona Delpuech,Stephen Fawell,David Fisher,Sladjana Gagrica,Eric Gangl,Tyler Grebe,Ryan David Robert Greenwood,Sudhir Hande,Holia Hatoum-Mokdad,Kara Herlihy,Samantha Hughes,Thomas A Hunt,Hoan Huynh,Sophie Janbon,Tony Johnson,Stefan Kavanagh,Teresa C M Klinowska,Mandy Lawson,Andrew Lister
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Aryloxy Diester Phosphonamidate Prodrugs of Phosphoantigens (ProPAgens) as Potent Activators of Vγ9/Vδ2 T-Cell Immune Responses. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-15 Hachemi Kadri,Taher E Taher,Qin Xu,Maria Sharif,Elizabeth Ashby,Richard T Bryan,Benjamin E Willcox,Youcef Mehellou
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Correction to Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity In Vivo J. Med. Chem. (IF 6.205) Pub Date : 2020-09-28 Claudia Mugnaini; Magdalena Kostrzewa; Marta Bryk; Ali Mokhtar Mahmoud; Antonella Brizzi; Stefania Lamponi; Gianluca Giorgi; Francesca Ferlenghi; Federica Vacondio; Paola Maccioni; Giancarlo Colombo; Marco Mor; Katarzyna Starowicz; Vincenzo Di Marzo; Alessia Ligresti; Federico Corelli
Page 7388. Marta Bryk’s affiliation should be “Department of Neurochemistry, Maj Institute of Pharmacology, Polish Academy of Sciences, ul. Smetna 12, 31-343 Cracow, Poland” instead of “Institute of Genetics and Biophysics, National Research Council of Italy, Via Pietro Castellino 111, 80131 Napoli, Italy”. Page 7388. Katarzyna Starowicz’s affiliation should be “Department of Neurochemistry, Maj Institute
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Pyrazole-Based Lactate Dehydrogenase (LDH) Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Ganesha Rai,Daniel J Urban,Bryan T Mott,Xin Hu,Shyh-Ming Yang,Gloria A Benavides,Michelle S Johnson,Giuseppe L Squadrito,Kyle R Brimacombe,Tobie D Lee,Dorian M Cheff,Hu Zhu,Mark J Henderson,Katherine Pohida,Gary A Sulikowski,David M Dranow,Md Kabir,Pranav Shah,Elias Padilha,Dingyin Tao,Yuhong Fang,Plamen P Christov,Kwangho Kim,Somnath Jana,Pavan Muttil,Tamara Anderson,Nitesh K Kunda,Helen J Hathaway
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Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-10 Kentaro Futatsugi,Aaron C Smith,Meihua Tu,Brian Raymer,Kay Ahn,Steven B Coffey,Matthew S Dowling,Dilinie P Fernando,Jemy A Gutierrez,Kim Huard,Jayasankar Jasti,Amit S Kalgutkar,John D Knafels,Jayvardhan Pandit,Kevin D Parris,Sylvie Perez,Jeffrey A Pfefferkorn,David A Price,Tim Ryder,Andre Shavnya,Ingrid A Stock,Andy S Tsai,Gregory J Tesz,Benjamin A Thuma,Yan Weng,Hanna Wisniewska,Gang Xing,Jun Zhou
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Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor J. Med. Chem. (IF 6.205) Pub Date : 2020-09-25 Jakub Gunera; Jillian G. Baker; Niek van Hilten; Daniel M. Rosenbaum; Peter Kolb
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Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-10 Matthew J LaMarche,Michael G Acker,Andreea Argintaru,Daniel Bauer,Julie Boisclair,Homan Chan,Christine Chen,Ying-Nan P Chen,Zhuoliang Chen,Zhan Deng,Michaël Doré,David Dunstan,Jianmei Fan,Peter Fekkes,Brant Firestone,Michelle Fodor,Jorge Garcia-Fortanet,Pascal D Fortin,Cary Fridrich,John Giraldes,Meir Glick,Denise Grunenfelder,Huia-Xiang Hao,Martin Hentemann,Samuel Ho,Andriana Jouk,Zhao B Kang,Rajesh
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Development of Bis-Cyclic Imidazolidine-4-one Derivatives as Potent Antibacterial Agents. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Minghui Wang,Ruixuan Gao,Mengmeng Zheng,Peng Sang,Chunpu Li,En Zhang,Qi Li,Jianfeng Cai
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Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-14 Chaoguo Cao,Jie Yang,Yong Chen,Peiting Zhou,Yingwei Wang,Wu Du,Lifeng Zhao,Yuanwei Chen
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Biased agonism at nociceptin/orphanin FQ receptors: a structure activity study on N/OFQ(1-13)-NH2. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Salvatore Pacifico,Federica Ferrari,Valentina Albanese,Erika Marzola,Joaquim Azevedo Neto,Chiara Ruzza,Girolamo Calo,Delia Preti,Remo Guerrini
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Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Frédéric Labéguère,Sonia Dupont,Luke Alvey,Florilène Soulas,Gregory Newsome,Amynata Tirera,Vanessa Quenehen,Thi Thu Trang Mai,Pierre Deprez,Roland Blanqué,Line Oste,Sandrine Le Tallec,Steve De Vos,Annick Hagers,Ann Vandevelde,Luc Nelles,Nele Vandervoort,Katja Conrath,Thierry Christophe,Ellen van der Aar,Emanuelle Wakselman,Didier Merciris,Céline Cottereaux,Cécile da Costa,Laurent Saniere,Philippe Clement-Lacroix
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Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3Kα and mTOR Kinases for the Treatment of Solid Tumors. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-08 Dinesh Mahajan,Somdutta Sen,Bilash Kuila,Amit Sharma,Reena Arora,Milind Sagar,Amal Ray Mahapatra,Lalita Babasaheb Gawade,Sundeep Dugar
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Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Simon Gonzalez,Maria Dumitrascuta,Emilie Eiselt,Stevany Louis,Linda Kunze,Annalisa Blasiol,Mélanie Vivancos,Santo Previti,Elke Dewolf,Charlotte Martin,Dirk Tourwè,Florine Cavelier,Louis Gendron,Philippe Sarret,Mariana Spetea,Steven Ballet
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DFG-1 Binding: A New Residue for Developing Selective Kinase Inhibitors. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Erik B Faber,Gunda I Georg
Only 15% of human kinases carry a bulky residue at the DFG-1 position, providing an opportunity for the design of selective ATP-site inhibitors without the typical hinge-binding interactions. The low sequence homology among unrelated kinases with bulky DFG-1 residues provides a new paradigm for selective kinase inhibitor development.
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DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-12 Martin Schröder,Alex N Bullock,Oleg Fedorov,Franz Bracher,Apirat Chaikuad,Stefan Knapp
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Anti-EGFR Fibronectin Bispecific Chemically Self-Assembling Nanorings (CSANs) Induce Potent T Cell-Mediated Antitumor Responses and Downregulation of EGFR Signaling and PD-1/PD-L1 Expression. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-27 Ozgun Kilic,Marcos R Matos de Souza,Abdulaziz A Almotlak,Yiao Wang,Jill M Siegfried,Mark D Distefano,Carston R Wagner
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Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-20 Satish Noonepalle,Sida Shen,Jakub Ptáček,Maurício T Tavares,Guiping Zhang,Jan Stránský,Jiří Pavlíček,Glaucio M Ferreira,Melissa Hadley,Guido Pelaez,Cyril Bařinka,Alan P Kozikowski,Alejandro Villagra
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Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-24 Andrea Shergalis,Ding Xue,Fatma Z Gharbia,Hannah Driks,Binita Shrestha,Amina Tanweer,Kirin Cromer,Mats Ljungman,Nouri Neamati
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Identification and Preclinical Development of a 2,5,6-Trisubstituted Fluorinated Pyridine Derivative as a Radioligand for the Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-11 Ahmed Haider,Luca Gobbi,Julian Kretz,Christoph Ullmer,Andreas Brink,Michael Honer,Thomas J Woltering,Dieter Muri,Hans Iding,Markus Bürkler,Martin Binder,Christian Bartelmus,Irene Knuesel,Pal Pacher,Adrienne Müller Herde,Francesco Spinelli,Hazem Ahmed,Kenneth Atz,Claudia Keller,Markus Weber,Roger Schibli,Linjing Mu,Uwe Grether,Simon M Ametamey
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Discovery of N-Arylsulfonyl-Indole-2-Carboxamide Derivatives as Potent, Selective, and Orally Bioavailable Fructose-1,6-Bisphosphatase Inhibitors-Design, Synthesis, In Vivo Glucose Lowering Effects, and X-ray Crystal Complex Analysis. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-21 Jie Zhou,Jianbo Bie,Xiaoyu Wang,Quan Liu,Rongcui Li,Hualong Chen,Jinping Hu,Hui Cao,Wenming Ji,Yan Li,Shuainan Liu,Zhufang Shen,Bailing Xu
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Bioinspired Hybrid Fluorescent Ligands for the FK1 Domain of FKBP52. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-31 Inès Li de la Sierra-Gallay,Mathilde Belnou,Béatrice Chambraud,Melanie Genet,Herman van Tilbeurgh,Magali Aumont-Nicaise,Michel Desmadril,Etienne-Emile Baulieu,Yves Jacquot,Cillian Byrne
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Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-17 Nina Reßing,Melf Sönnichsen,Jeremy D Osko,Andrea Schöler,Julian Schliehe-Diecks,Alexander Skerhut,Arndt Borkhardt,Julia Hauer,Matthias U Kassack,David W Christianson,Sanil Bhatia,Finn K Hansen
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Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Hideki Furukawa,Yasufumi Miyamoto,Yasuhiro Hirata,Koji Watanabe,Yuko Hitomi,Yayoi Yoshitomi,Jumpei Aida,Naoyoshi Noguchi,Nobuyuki Takakura,Kazuaki Takami,Seiji Miwatashi,Yoshihiko Hirozane,Teruki Hamada,Ryo Ito,Mitsugi Ookawara,Yusuke Moritoh,Masanori Watanabe,Tsuyoshi Maekawa
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Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of AL-611 as an HCV NS5B Polymerase Inhibitor for the Treatment of Chronic Hepatitis C. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-20 Guangyi Wang,Natalia Dyatkina,Marija Prhavc,Caroline Williams,Vladimir Serebryany,Yujian Hu,Yongfei Huang,Xiangyang Wu,Tongqian Chen,Wensheng Huang,Vivek K Rajwanshi,Jerome Deval,Amy Fung,Zhinan Jin,Antitsa Stoycheva,Kenneth Shaw,Kusum Gupta,Yuen Tam,Andreas Jekle,David B Smith,Leonid Beigelman
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Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-27 Satoshi Endo,Hiroaki Oguri,Jin Segawa,Mina Kawai,Dawei Hu,Shuang Xia,Takuya Okada,Katsumasa Irie,Shinya Fujii,Hiroaki Gouda,Kazuhiro Iguchi,Takuo Matsukawa,Naohiro Fujimoto,Toshiyuki Nakayama,Naoki Toyooka,Toshiyuki Matsunaga,Akira Ikari
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Superior Pyrimidine Derivatives as Selective ABCG2 Inhibitors and Broad-Spectrum ABCB1, ABCC1, and ABCG2 Antagonists. J. Med. Chem. (IF 6.205) Pub Date : 2020-07-31 Katja Silbermann,Jiyang Li,Vigneshwaran Namasivayam,Fabian Baltes,Gerd Bendas,Sven Marcel Stefan,Michael Wiese
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Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-31 Xiaohui Du,Jared Moore,Brian R Blank,John Eksterowicz,Dena Sutimantanapi,Natalie Yuen,Todd Metzger,Brenda Chan,Tom Huang,Xi Chen,Yuping Chen,Frank Duong,Wayne Kong,Jae H Chang,Jessica Sun,Tatiana Zavorotinskaya,Qiuping Ye,Melissa R Junttila,Chudi Ndubaku,Lori S Friedman,Valeria R Fantin,Daqing Sun
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Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-17 Sébastien L Degorce,Omid Tavana,Erica Banks,Claire Crafter,Lakshmaiah Gingipalli,David Kouvchinov,Yumeng Mao,Fiona Pachl,Anisha Solanki,Viia Valge-Archer,Bin Yang,Scott D Edmondson
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Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-12 Xiuli Chen,Weining Sun,Shenzhen Huang,Hailin Zhang,Guifeng Lin,Hui Li,Jingxin Qiao,Linli Li,Shengyong Yang
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New Polyaminoisoprenyl Antibiotics Enhancers against Two Multidrug-Resistant Gram-Negative Bacteria from Enterobacter and Salmonella Species. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-25 Aurélie Lieutaud,Cyril Pieri,Jean Michel Bolla,Jean Michel Brunel
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XGen: Real-Space Fitting of Complex Ligand Conformational Ensembles to X-ray Electron Density Maps. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-02 Ajay N Jain,Ann E Cleves,Alexander C Brueckner,Charles A Lesburg,Qiaolin Deng,Edward C Sherer,Mikhail Y Reibarkh
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Correction to Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-14 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,Mercè Pallàs,Luis F Callado
Page 3630. The affiliation of the following authors needs to be corrected. Iria Brocos-Mosquera is affiliated with Department of Pharmacology, University of the Basque Country, UPV/EHU, E-48940 Leioa, Bizkaia, Spain, and Centro de Investigación Biomédica en Red de Salud Mental, CIBERSAM, Spain. Carolina Muguruza is affiliated with Department of Pharmacology, University of the Basque Country, UPV/EHU
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Correction to Peptide-β-lactam Inhibitors of Dengue and West Nile Virus NS2B-NS3 Protease Display Two Distinct Binding Modes. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-01 Tonko Dražić,Sara Kopf,James Corridan,Mila M Leuthold,Branimir Bertoša,Christian D Klein
Page 140. In the graphical abstract, the blue curved arrow starting from the enzyme should point to the lysine carbonyl group instead of the benzyloxyphenylglycine carbonyl group. The correct image is shown below. Page 154. In the Acknowledgments, a sentence “The manuscript has been published open access with the support of the Marie Curie Alumni Association.” should be added. This article has not
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Correction to Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-01 Anthony Knight,Jennifer L Hemmings,Ian Winfield,Michele Leuenberger,Eugenia Frattini,Bruno G Frenguelli,Simon J Dowell,Martin Lochner,Graham Ladds
Page 952. The structural formula of CCPA immediately below the Table 1 title should be This article has not yet been cited by other publications.
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Correction to "Bifunctional Naphtho[2,3-d][1,2,3]triazole-4,9-dione Compounds Exhibit Antitumor Effects In Vitro and In Vivo by Inhibiting Dihydroorotate Dehydrogenase and Inducing Reactive Oxygen Species Production". J. Med. Chem. (IF 6.205) Pub Date : 2020-09-14 Zeping Zuo,Xiaocong Liu,Xinying Qian,Ting Zeng,Na Sang,Huan Liu,Yue Zhou,Lei Tao,Xia Zhou,Na Su,Yamei Yu,Qiang Chen,Youfu Luo,Yinglan Zhao
The following reference citation should be added to “the previous step”: Ramachary, D. B.; Shashank, A. B.; Karthik, S. An organocatalytic Azide–Aldehyde [3 + 2] Cycloaddition: High-Yielding Regioselective Synthesis of 1,4-Disubstituted 1,2,3-Triazoles. Angew. Chem., Int. Ed. 2014, 53, 10420–10424. (DOI: 10.1002/anie.201406721. Published on July 30, 2014). This article has not yet been cited by other
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Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT1A Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-04 Joanna Sniecikowska,Monika Gluch-Lutwin,Adam Bucki,Anna Więckowska,Agata Siwek,Magdalena Jastrzebska-Wiesek,Anna Partyka,Daria Wilczyńska,Karolina Pytka,Gniewomir Latacz,Katarzyna Przejczowska-Pomierny,Elżbieta Wyska,Anna Wesołowska,Maciej Pawłowski,Adrian Newman-Tancredi,Marcin Kolaczkowski
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Therapeutic Exploitation of GPR18: Beyond the Cannabinoids? J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Paula Morales,Ana Lago-Fernandez,Dow P Hurst,Noori Sotudeh,Eugen Brailoiu,Patricia H Reggio,Mary E Abood,Nadine Jagerovic
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Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Takeshi Yokoyama,Mineyuki Mizuguchi
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Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-01 Patrick Mäder,Lars Kattner
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Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-16 Magdalena Konieczny,Bogdan Musielak,Justyna Kocik,Lukasz Skalniak,Dominik Sala,Miroslawa Czub,Katarzyna Magiera-Mularz,Ismael Rodriguez,Maja Myrcha,Malgorzata Stec,Maciej Siedlar,Tad A Holak,Jacek Plewka
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Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-04 Laura Cooper,Adam Schafer,Yangfeng Li,Han Cheng,Bani Medegan Fagla,Zhengnan Shen,Raghad Nowar,Katherine Dye,Manu Anantpadma,Robert A Davey,Gregory R J Thatcher,Lijun Rong,Rui Xiong
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Discovery of Novel Pyrazolo[3,4-b] Pyridine Derivatives with Dual Activities of Vascular Remodeling Inhibition and Vasodilation for the Treatment of Pulmonary Arterial Hypertension. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-11 Liqing Hu,Lijun Li,Qi Chang,Songsen Fu,Jia Qin,Zhuo Chen,Xiaohui Li,Qinglian Liu,Gaoyun Hu,Qianbin Li
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Development of PSMA-1007-Related Series of 18F-Labeled Glu-Ureido-Type PSMA Inhibitors. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-27 Jens Cardinale,Mareike Roscher,Martin Schäfer,Max Geerlings,Martina Benešová,Ulrike Bauder-Wüst,Yvonne Remde,Matthias Eder,Zora Nováková,Lucia Motlová,Cyril Barinka,Frederik L Giesel,Klaus Kopka
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Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2). J. Med. Chem. (IF 6.205) Pub Date : 2020-09-22 Tomoteru Yamasaki,Xiaofei Zhang,Katsushi Kumata,Yiding Zhang,Xiaoyun Deng,Masayuki Fujinaga,Zhen Chen,Wakana Mori,Kuan Hu,Hidekatsu Wakizaka,Akiko Hatori,Lin Xie,Masanao Ogawa,Nobuki Nengaki,Richard Van,Yihan Shao,Douglas J Sheffler,Nicholas D P Cosford,Steven H Liang,Ming-Rong Zhang
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Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ). J. Med. Chem. (IF 6.205) Pub Date : 2020-09-04 Konstantin Hinnah,Sabine Willems,Johannes Morstein,Jan Heering,Felix W W Hartrampf,Johannes Broichhagen,Philipp Leippe,Daniel Merk,Dirk Trauner
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Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-03 Khoubaib Ben Haj Salah,Mathieu Maingot,Anne-Laure Blayo,Céline M'Kadmi,Marjorie Damian,Sophie Mary,Sonia Cantel,Jérémie Neasta,Catherine Oiry,Sylvie Péraldi-Roux,Gimena Fernandez,Guadalupe García Romero,Mario Perello,Jacky Marie,Jean-Louis Banères,Jean-Alain Fehrentz,Séverine Denoyelle
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Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-08 Tong Zhao,Qing Meng,Zhuosen Sun,Yanyu Chen,Wei Ai,Zean Zhao,Dongwei Kang,Yue Dong,Ruipeng Liang,Ting Wu,Jianxin Pang,Xinyong Liu,Peng Zhan
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Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-26 Haixia Sun,Daoyuan Chen,Siyue Zhan,Weijian Wu,Huiying Xu,Chunxiang Luo,Hui Su,Yanqiao Feng,Weiyan Shao,Arabella Wan,Binhua Zhou,Guohui Wan,Xianzhang Bu
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Bifunctional and Unusual Amino Acid β- or γ-Ester Prodrugs of Nucleoside Analogues for Improved Affinity to ATB0,+ and Enhanced Metabolic Stability: An Application to Floxuridine. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-03 Yongbing Sun,Yu Ke,Chunshi Li,Jian Wang,Liangxing Tu,Lvjiang Hu,Yi Jin,Hao Chen,Jianping Gong,Zhiqiang Yu
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DPAGT1 Inhibitors of Capuramycin Analogues and Their Antimigratory Activities of Solid Tumors. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-04 Katsuhiko Mitachi,Rita G Kansal,Kirk E Hevener,Cody D Gillman,Syed M Hussain,Hyun Gi Yun,Gustavo A Miranda-Carboni,Evan S Glazer,William M Clemons,Michio Kurosu
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Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting. J. Med. Chem. (IF 6.205) Pub Date : 2020-08-18 Kim Huard,Aaron C Smith,Gregg Cappon,Robert L Dow,David J Edmonds,Ayman El-Kattan,William P Esler,Dilinie P Fernando,David A Griffith,Amit S Kalgutkar,Trenton T Ross,Scott W Bagley,David Beebe,Yi-An Bi,Shawn Cabral,Collin Crowley,Shawn D Doran,Matthew S Dowling,Spiros Liras,Vincent Mascitti,Mark Niosi,Jeffrey A Pfefferkorn,Jana Polivkova,Cathy Préville,David A Price,Andre Shavnya,Norimitsu Shirai,Andrew
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Recent Advances on Nitrones Design for Stroke Treatment. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-01 José Marco-Contelles
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Catch and Anchor Approach To Combat Both Toxicity and Longevity of Botulinum Toxin A. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-04 Lucy Lin,Margaret E Olson,Takashi Sugane,Lewis D Turner,Margarita A Tararina,Alexander L Nielsen,Elbek K Kurbanov,Sabine Pellett,Eric A Johnson,Seth M Cohen,Karen N Allen,Kim D Janda
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Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-18 Nicoletta Brindani,Ambra Gianotti,Simone Giovani,Francesca Giacomina,Paolo Di Fruscia,Federico Sorana,Sine Mandrup Bertozzi,Giuliana Ottonello,Luca Goldoni,Ilaria Penna,Debora Russo,Maria Summa,Rosalia Bertorelli,Loretta Ferrera,Emanuela Pesce,Elvira Sondo,Luis J V Galietta,Tiziano Bandiera,Nicoletta Pedemonte,Fabio Bertozzi
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Synthesis and Evaluation of 4-Hydroxycoumarin Imines as Inhibitors of Class II Myosins. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-07 Jhonnathan Brawley,Emily Etter,Dante Heredia,Amarawan Intasiri,Kyle Nennecker,Joshua Smith,Brandon M Welcome,Richard K Brizendine,Thomas W Gould,Thomas W Bell,Christine Cremo
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Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors. J. Med. Chem. (IF 6.205) Pub Date : 2020-09-09 Hai-Shan Zhou,Lv-Bin Hu,Han Zhang,Wen-Xin Shan,Yan Wang,Xue Li,Tian Liu,Jing Zhao,Qi-Dong You,Zheng-Yu Jiang
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