Literature DB >> 17485205

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.

Timothy I Richardson1, Bryan H Norman, Charles W Lugar, Scott A Jones, Yong Wang, Jim D Durbin, Venkatesh Krishnan, Jeffrey A Dodge.   

Abstract

Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe structure-activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures of 5b and a non-selective analog 5c in ERalpha help explain the observed selectivity of the benzopyran platform.

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Year:  2007        PMID： 17485205     DOI： 10.1016/j.bmcl.2007.04.051

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


  6 in total

1.  Selective estrogen receptor modulators regulate stromal proliferation in human benign prostatic hyperplasia by multiple beneficial mechanisms--action of two new agents.

Authors:  Rajeev Kumar; Vikas Verma; Amit Sarswat; J P Maikhuri; Ashish Jain; Rajeev K Jain; V L Sharma; Diwakar Dalela; Gopal Gupta
Journal:  Invest New Drugs       Date:  2010-12-23       Impact factor: 3.850

2.  Functionalized cyclopentenes through a tandem NHC-catalyzed dynamic kinetic resolution and ambient temperature decarboxylation: mechanistic insight and synthetic application.

Authors:  Daniel T Cohen; Ryne C Johnston; Nicholas T Rosson; Paul Ha-Yeon Cheong; Karl A Scheidt
Journal:  Chem Commun (Camb)       Date:  2015-02-14       Impact factor: 6.222

3.  Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta.

Authors:  Michael Waibel; Meri De Angelis; Fabio Stossi; Karen J Kieser; Kathryn E Carlson; Benita S Katzenellenbogen; John A Katzenellenbogen
Journal:  Eur J Med Chem       Date:  2009-02-20       Impact factor: 6.514

4.  Tricyclic flavonoids with 1,3-dithiolium substructure.

Authors:  Lucian G Bahrin; Peter G Jones; Henning Hopf
Journal:  Beilstein J Org Chem       Date:  2012-11-16       Impact factor: 2.883

5.  Docking study of triphenylphosphonium cations as estrogen receptor alpha modulators.

Authors:  Joseph P Salisbury; John C Williams
Journal:  Bioinformation       Date:  2009-02-28

Review 6.  Versatility or promiscuity: the estrogen receptors, control of ligand selectivity and an update on subtype selective ligands.

Authors:  Hui Wen Ng; Roger Perkins; Weida Tong; Huixiao Hong
Journal:  Int J Environ Res Public Health       Date:  2014-08-26       Impact factor: 3.390
  6 in total

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