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

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

  • Bioorg Med Chem Lett. 2010 Jan 1;20(1):272-5. doi: 10.1016/j.bmcl.2009.10.111.
Koichiro Harada 1,  Hideki Kubo,  Yoshitaka Tomigahara,  Kazuhiko Nishioka,  Junya Takahashi,  Mio Momose,  Shinichi Inoue,  Atsuyuki Kojima
Affiliations

Affiliation

  • 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
PMID: 19954971 DOI: 10.1016/j.bmcl.2009.10.111
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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