Literature DB >> 23403081

Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives.

Rui Wang1, Hong-Fan Shi, Jing-Feng Zhao, Yan-Ping He, Hong-Bin Zhang, Jian-Ping Liu.   

Abstract

A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23403081     DOI: 10.1016/j.bmcl.2013.01.045

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


  4 in total

Review 1.  Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.

Authors:  Debashis Ghosh; Jessica Lo; Chinaza Egbuta
Journal:  J Med Chem       Date:  2016-01-19       Impact factor: 7.446

2.  Structure-activity relationships and docking studies of synthetic 2-arylindole derivatives determined with aromatase and quinone reductase 1.

Authors:  Allan M Prior; Xufen Yu; Eun-Jung Park; Tamara P Kondratyuk; Yan Lin; John M Pezzuto; Dianqing Sun
Journal:  Bioorg Med Chem Lett       Date:  2017-11-06       Impact factor: 2.823

3.  Towards an Understanding of the Mode of Action of Human Aromatase Activity for Azoles through Quantum Chemical Descriptors-Based Regression and Structure Activity Relationship Modeling Analysis.

Authors:  Chayawan Chayawan; Cosimo Toma; Emilio Benfenati; Ana Y Caballero Alfonso
Journal:  Molecules       Date:  2020-02-08       Impact factor: 4.411

4.  Rational Development of a Potent 15-Lipoxygenase-1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties.

Authors:  Nikolaos Eleftheriadis; Constantinos G Neochoritis; Niek G J Leus; Petra E van der Wouden; Alexander Dömling; Frank J Dekker
Journal:  J Med Chem       Date:  2015-09-16       Impact factor: 7.446

  4 in total

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