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ACS Med Chem Lett. 2010 Oct 22;2(1):2-6. doi: 10.1021/ml100071j. eCollection 2011 Jan 13.

First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.

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Pharmaceutical and Medicinal Chemistry, Saarland University & Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Campus C2 3, D-66123 Saarbrücken, Germany.


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).


CYP11B1 inhibitor; CYP11B2; CYP17; CYP19; Cushing's syndrome; etomidate; steroid hormone biosynthesis; steroid-11β-hydroxylase

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