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Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis

JOURNAL ARTICLE published 14 January 2021 in Journal of Medicinal Chemistry

Authors: 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

Issue Editorial Masthead

JOURNAL ARTICLE published 11 April 2024 in Journal of Medicinal Chemistry

Design of Novel 2-Phenylquinazolin-4-amines as Selective CYP1B1 Inhibitors for Overcoming Paclitaxel Resistance in A549 Cells

JOURNAL ARTICLE published 11 April 2024 in Journal of Medicinal Chemistry

Research funded by National Natural Science Foundation of China (22371026,82001869) | Creative Research Group of CQ University (CXQT21017) | Science and Technology Research Program of Chongqing Municipal Education Commission (KJQN202200446)

Authors: Meixian Yang | Fengyuan Yang | Xinyue Huang | Jiajing Cai | Yuxin Zhang | Jianhua Jia | Dachuan Qiu

CBP/p300 Degrader: A Promising Therapeutic Strategy for Treatment of Prostate Cancer and Beyond

JOURNAL ARTICLE published 11 April 2024 in Journal of Medicinal Chemistry

Authors: Jiankang Hu | Yong Xu

Discovery of Near-Infrared Heptamethine Cyanine Probes for Imaging-Guided Surgery in Solid Tumors

JOURNAL ARTICLE published 11 April 2024 in Journal of Medicinal Chemistry

Research funded by Jiangsu Planned Projects for Postdoctoral Research Funds (2023ZB521) | National Key Research and Development Program of China (2022YFE0138800) | Natural Science Foundation of Jiangsu Province (BE2023842) | Fundamental Research Funds for the Central Universities (2632023GR01) | National Natural Science Foundation of China (82230070)

Authors: Qiao Lin | Changsheng Li | Yuhua Wang | Yanqing Zhu | Yueqing Gu

Discovery of Novel 1,3,8-Triazaspiro[4.5]decane Derivatives That Target the c Subunit of F1/FO-Adenosine Triphosphate (ATP) Synthase for the Treatment of Reperfusion Damage in Myocardial Infarction

JOURNAL ARTICLE published 23 August 2018 in Journal of Medicinal Chemistry

Research funded by Universit? degli Studi di Ferrara (FIR1679708) | Fondazione Telethon (GGP15219/B) | Associazione Italiana per la Ricerca sul Cancro (IG-19803,IG-18624) | Narodowe Centrum Nauki (UMO-2014/15/B/NZ1/00490) | Ministero della Salute (GGP15219/B)

Authors: Giampaolo Morciano | Delia Preti | Gaia Pedriali | Giorgio Aquila | Sonia Missiroli | Anna Fantinati | Natascia Caroccia | Salvatore Pacifico | Massimo Bonora | Anna Talarico | Claudia Morganti | Paola Rizzo | Roberto Ferrari | Mariusz R. Wieckowski | Gianluca Campo | Carlotta Giorgi | Claudio Trapella | Paolo Pinton

Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing

JOURNAL ARTICLE published 10 December 2020 in Journal of Medicinal Chemistry

Authors: Carole Pissot Soldermann | Oliver Simic | Martin Renatus | Paulus Erbel | Samu Melkko | Markus Wartmann | Marc Bigaud | Andreas Weiss | Paul McSheehy | Ralf Endres | Paulo Santos | Jutta Blank | Ansgar Schuffenhauer | Guido Bold | Nicole Buschmann | Thomas Zoller | Eva Altmann | Paul W. Manley | Ina Dix | Elisabeth Buchdunger | Julien Scesa | Jean Quancard | Achim Schlapbach | Frédéric Bornancin | Thomas Radimerski | Catherine H. Régnier

Antimalarials. 7. Bis(trifluoromethyl)-.alpha.-(2-piperidyl)-4-quinolinemethanols

JOURNAL ARTICLE published October 1971 in Journal of Medicinal Chemistry

Authors: R. E. Lutz | C. J. Ohnmacht | A. R. Patel

Propofol Analogues. Synthesis, Relationships between Structure and Affinity at GABAAReceptor in Rat Brain, and Differential Electrophysiological Profile at Recombinant Human GABAAReceptors

JOURNAL ARTICLE published 1 May 1998 in Journal of Medicinal Chemistry

Authors: Giuseppe Trapani | Andrea Latrofa | Massimo Franco | Cosimo Altomare | Enrico Sanna | Marcello Usala | Giovanni Biggio | Gaetano Liso

4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines

JOURNAL ARTICLE published 24 December 2020 in Journal of Medicinal Chemistry

Research funded by Deutsche Forschungsgemeinschaft (CRC 992,EXC-2189,GU1225/3-1,WO2012/1-1)

Authors: Martin Hügle | Pierre Regenass | Robin Warstat | Mirjam Hau | Karin Schmidtkunz | Xavier Lucas | Daniel Wohlwend | Oliver Einsle | Manfred Jung | Bernhard Breit | Stefan Günther

Identification of a New Class of Glucokinase Activators through Structure-Based Design

JOURNAL ARTICLE published 10 October 2013 in Journal of Medicinal Chemistry

Authors: Ronald J. Hinklin | Steven A. Boyd | Mark J. Chicarelli | Kevin R. Condroski | Walter E. DeWolf | Patrice A. Lee | Waiman Lee | Ajay Singh | Laurie Thomas | Walter C. Voegtli | Lance Williams | Thomas D. Aicher

Leaving Groups Prolong the Duration of 20S Proteasome Inhibition and Enhance the Potency of Salinosporamides

JOURNAL ARTICLE published 13 November 2008 in Journal of Medicinal Chemistry

Authors: Rama Rao Manam | Katherine A. McArthur | Ta-Hsiang Chao | Jeffrey Weiss | Janid A. Ali | Vito J. Palombella | Michael Groll | G. Kenneth Lloyd | Michael A. Palladino | Saskia T. C. Neuteboom | Venkat R. Macherla | Barbara C. M. Potts

Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogs of piceatannol

JOURNAL ARTICLE published October 1993 in Journal of Medicinal Chemistry

Authors: Kshitij Thakkar | Robert L. Geahlen | Mark Cushman

Synthesis and Structure–Activity Relationship (SAR) Studies of Novel Pyrazolopyridine Derivatives as Inhibitors of Enterovirus Replication

JOURNAL ARTICLE published 22 February 2018 in Journal of Medicinal Chemistry

Research funded by National Institute of Allergy and Infectious Diseases (AI-107383)

Authors: Yanpeng Xing | Jun Zuo | Paul Krogstad | Michael E. Jung

Rationally Designed High-Affinity 2-Amino-6-halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity

JOURNAL ARTICLE published 1 June 2007 in Journal of Medicinal Chemistry

Authors: Srinivas R. Kasibhatla | Kevin Hong | Marco A. Biamonte | David J. Busch | Patricia L. Karjian | John L. Sensintaffar | Adeela Kamal | Rachel E. Lough | John Brekken | Karen Lundgren | Roy Grecko | Gregg A. Timony | Yingqing Ran | Robert Mansfield | Lawrence C. Fritz | Edgar Ulm | Francis J. Burrows | Marcus F. Boehm

Synthesis and Structure−Activity Relationships of 3,7-Dimethyl-1-propargylxanthine Derivatives, A2A-Selective Adenosine Receptor Antagonists

JOURNAL ARTICLE published 1 December 1997 in Journal of Medicinal Chemistry

Authors: Christa E. Müller | Uli Geis | Jo Hipp | Ulrike Schobert | Wolfram Frobenius | Maciej Pawłowski | Fumio Suzuki | Jesús Sandoval-Ramírez

Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective

JOURNAL ARTICLE published 24 December 2020 in Journal of Medicinal Chemistry

Research funded by Ministry of Education of the People's Republic of China (CPU2018GY07) | National Natural Science Foundation of China (21372260,21672260,82073702) | State Key Laboratory of Drug Research (SIMM1903KF-03)

Authors: Xi Feng | Dongdong Liao | Dongyu Liu | An Ping | Zhiyu Li | Jinlei Bian

Structure-activity relationship studies at benzodiazepine receptor (BZR): a comparison of the substituent effects of pyrazoloquinolinone analogs

JOURNAL ARTICLE published May 1993 in Journal of Medicinal Chemistry

Authors: R. Ian Fryer | Puwen Zhang | Roberto Rios | Zi Qiang Gu | Anthony S. Basile | Phil Skolnick

New Multifunctional Di-tert-butylphenoloctahydro(pyrido/benz)oxazine Derivatives with Antioxidant, Antihyperlipidemic, and Antidiabetic Action

JOURNAL ARTICLE published 25 April 2013 in Journal of Medicinal Chemistry

Authors: Eleni Ladopoulou | Alexios N. Matralis | Angeliki P. Kourounakis

7-Substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials

JOURNAL ARTICLE published March 1988 in Journal of Medicinal Chemistry

Authors: John M. Domagala | Susan E. Hagen | Carl L. Heifetz | Marland P. Hutt | Thomas F. Mich | Joseph P. Sanchez | Ashok K. Trehan