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

K Harada, H Kubo, Y Tomigahara, K Nishioka…

Index: Harada, Koichiro; Kubo, Hideki; Tomigahara, Yoshitaka; Nishioka, Kazuhiko; Takahashi, Junya; Momose, Mio; Inoue, Shinichi; Kojima, Atsuyuki Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 272 - 275

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Citation Number: 30

Abstract

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

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