期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 2, 期 1, 页码 2-6出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100071J
关键词
Cushing's syndrome; steroid hormone biosynthesis; steroid-11 beta-hydroxylase; CYP11B1 inhibitor; CYP17; CYP19; CYP11B2; etomidate
资金
- European Postgraduate School 532 (DFG)
Outgoing from an etomidate-based design concept, we succeeded in the development of a series of highly active and selective inhibitors of CYP11B1, the key enzyme of cortisol biosynthesis, as potential drugs for the treatment of Cushing's syndrome and related diseases. Thus, compound 33 (IC50 = 152 nM) is the first CYP11B1 inhibitor showing a rather good selectivity toward the most important steroidogenic CYP enzymes aldosterone synthase (CYP11B2), the androgen-forming CYP17, and aromatase (estrogen synthase, CYP19).
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