Literature DB >> 19664922

2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists.

Yonghui Wang1, Chaya Duraiswami, Kevin P Madauss, Thuy B Tran, Shawn P Williams, Su-Jun Deng, Todd L Graybill, Marlys Hammond, David G Jones, Eugene T Grygielko, Jeffrey D Bray, Scott K Thompson.   

Abstract

High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and selective agonists 9 and 11, X-ray crystal structure of 9 bound to PR-LBD and preliminary developability data are described.

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Year:  2009        PMID: 19664922     DOI: 10.1016/j.bmcl.2009.07.100

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.

Authors:  Fraser F Fleming; Lihua Yao; P C Ravikumar; Lee Funk; Brian C Shook
Journal:  J Med Chem       Date:  2010-08-30       Impact factor: 7.446

2.  Predicting the reactivity of nitrile-carrying compounds with cysteine: a combined computational and experimental study.

Authors:  Anna Berteotti; Federica Vacondio; Alessio Lodola; Michele Bassi; Claudia Silva; Marco Mor; Andrea Cavalli
Journal:  ACS Med Chem Lett       Date:  2014-02-24       Impact factor: 4.345

  2 in total

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