Literature DB >> 9871704

Design and synthesis of a new type of non steroidal human aromatase inhibitors.

P Sonnet1, J Guillon, C Enguehard, P Dallemagne, R Bureau, P Rault S Auvray, S Moslemi, P Sourdiane, S Galopin, G E Séralini.   

Abstract

The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1 (MR20814), allowed us to design some related derivatives as potential new inhibitors. Among those we synthesized, chlorophenylpyridylmethylenetetrahydroindolizinone 5 (MR20492) exhibited in vitro a ten-fold higher inhibition of the enzyme (IC50 = 0.2 +/- 0.0 microM and Ki = 10.3 +/- 3.3 nM).

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Year:  1998        PMID: 9871704     DOI: 10.1016/s0960-894x(98)00157-7

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


  3 in total

1.  Docking and 3D-QSAR studies of diverse classes of human aromatase (CYP19) inhibitors.

Authors:  Partha Pratim Roy; Kunal Roy
Journal:  J Mol Model       Date:  2010-03-01       Impact factor: 1.810

2.  Enantioselective synthesis of polycyclic nitrogen heterocycles by Rh-catalyzed alkene hydroacylation: constructing six-membered rings in the absence of chelation assistance.

Authors:  Xiang-Wei Du; Avipsa Ghosh; Levi M Stanley
Journal:  Org Lett       Date:  2014-07-14       Impact factor: 6.005

Review 3.  In Silico Prediction of Chemical Toxicity for Drug Design Using Machine Learning Methods and Structural Alerts.

Authors:  Hongbin Yang; Lixia Sun; Weihua Li; Guixia Liu; Yun Tang
Journal:  Front Chem       Date:  2018-02-20       Impact factor: 5.221

  3 in total

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