Document Report Card

ID: ALA1649094

Journal: ACS Med Chem Lett

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

Authors: Hille UE, Zimmer C, Vock CA, Hartmann RW.

Abstract: 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).

CiteXplore: 24900247

DOI: 10.1021/ml100071j