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

Bioorganic & medicinal chemistry letters (2009-12-04)
Koichiro Harada, Hideki Kubo, Yoshitaka Tomigahara, Kazuhiko Nishioka, Junya Takahashi, Mio Momose, Shinichi Inoue, Atsuyuki Kojima
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
4-Methylumbelliferone, ≥98%
Sigma-Aldrich
7-Hydroxy-4-(trifluoromethyl)coumarin, 98%

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