Androsterone 3β-substituted derivatives as inhibitors of type 3 17β-hydroxysteroid dehydrogenase

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作者
Ngatcha, BT
Luu-The, V
Poirier, D
机构
[1] Univ Laval, CHUL, Med Ctr, Oncol & Mol Endocrinol Res Ctr,Div Med Chem, Quebec City, PQ G1V 4G2, Canada
[2] Univ Laval, CHUL, Med Ctr, MRC,Grp Mol Endocrinol, Quebec City, PQ G1V 4G2, Canada
[3] Univ Laval, CHUL, Med Ctr, Oncol & Mol Endocrinol Res Ctr, Quebec City, PQ G1V 4G2, Canada
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Androsterone derivatives substituted at position 3 were synthesized starting from dihydrotestosterone in a short sequence of reactions. They proved to be potent inhibitors (IC50 = 57-147 nM) of type 3 17 beta -hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transformation of androstenedione to steroid active androgen testosterone. (C) 2000 Elsevier Science Ltd. All rights reserved.
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页码:2533 / 2536
页数:4
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