1361475-29-7Relevant academic research and scientific papers
Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17β-HSD1
Spadaro, Alessandro,Frotscher, Martin,Hartmann, Rolf W.
supporting information; experimental part, p. 2469 - 2473 (2012/05/20)
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.
