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KMID : 0370220100540060466
Yakhak Hoeji
2010 Volume.54 No. 6 p.466 ~ p.473
Synthesis and -Reductase Inhibitory Activity of -Substituted 5-Androstene-17-Carboxamides
Jo Ik-Sung

Ma Eun-Sook
Abstract
A series of -substituted 5-androstene--carboxamides were synthesized from analogs of -hydroxy-5-androstene--carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone -reductase inhibitory activity of synthesized compounds was assessed by radioimmunoassay using [1,2,6,7-3H]-testosterone as substrate. All synthesized compounds showed lower activity than finasteride and the N-(3-pyridino)--carboxycarbonyloxy-5-androstene--carboxamide (12) showed weak inhibitory activity (: ).
KEYWORD
-reductase inhibitor, prostate cancer, benign prostatic hyperplasia, -substituted 5-androstene--carboxamide
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