- Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17β-HSD1
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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.
- Spadaro, Alessandro,Frotscher, Martin,Hartmann, Rolf W.
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supporting information; experimental part
p. 2469 - 2473
(2012/05/20)
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- SELECTIVE 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS
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The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitors their production and use, especially for the treatment and/or prophylaxis of hormone-related diseases.
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Page/Page column 101-102
(2012/03/26)
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