Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.

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Abstract

The synthesis and SAR studies of 3- and 4-substituted 7-hydroxycoumarins as novel 17beta-HSD3 inhibitors are discussed. The most potent compounds from this series exhibited low nanomolar inhibitory activity with acceptable selectivity versus other 17beta-HSD isoenzymes and nuclear receptors.

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Journal

Journal ID (iso-abbrev): Bioorg. Med. Chem. Lett.

Title: Bioorganic & medicinal chemistry letters

ISSN (Electronic): 1464-3405

ISSN (Print): 0960-894X

Publication date (Electronic): Jan 1 2010

Volume: 20

Issue: 1

Affiliations

[1 ] Environmental Health Science Laboratory, Sumitomo Chemical Co., Ltd, 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-8558, Japan. haradak@sc.sumitomo-chem.co.jp

Article

Publisher Item ID: S0960-894X(09)01532-7

DOI: 10.1016/j.bmcl.2009.10.111

PubMed ID: 19954971

SO-VID: 62d534aa-a525-4e86-8585-7d5f0e715d61

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