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J Med Chem. 2012 Mar 8;55(5):2469-73. doi: 10.1021/jm201711b. Epub 2012 Feb 23.

Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17β-HSD1.

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1
Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.

Abstract

17β-HSD1 is a novel target for the treatment of estrogen-dependent diseases, as it catalyzes intracellular estradiol formation. Starting from two recently described compounds, highly active and selective inhibitors were developed. Benzoyl 6 and benzamide 17 are the most selective compounds toward 17β-HSD2 described so far. They also showed a promising profile regarding activity in T47-D cells, selectivity toward ERα and ERβ, inhibition of hepatic CYP enzymes, metabolic stability, and inhibition of marmoset 17β-HSD1 and 17β-HSD2.

PMID:
22277094
DOI:
10.1021/jm201711b
[Indexed for MEDLINE]

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