- 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.
Bioorganic & medicinal chemistry letters (2009-12-04)
Koichiro Harada, Hideki Kubo, Yoshitaka Tomigahara, Kazuhiko Nishioka, Junya Takahashi, Mio Momose, Shinichi Inoue, Atsuyuki Kojima
PMID19954971
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