期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 14, 页码 6629-6633出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm3003872
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CYP11B1 inhibition is a promising therapy for Cushing's syndrome. Starting from etomidate, references I and II, the title compounds were designed and synthesized. Cyclopropyl analogue 4 was identified as a CYP11B1 inhibitor more potent (IC50 = 2.2 nM) than leads and more selective (SF = 11) than I and metyrapone. Since it also showed potent inhibition of rat CYP11B1 and good selectivity over human CYP17 and CYP19, it is a promising candidate for further development.
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