3β-치환 5-Androstene-17-Carboxamides 합성과 5α-Reductase 저해 활성

• 영문명: Synthesis and 5α-Reductase Inhibitory Activity of 3β-Substituted 5-Androstene-17-Carboxamides
• 발행기관: 대한약학회
• 저자명: 조익성(Iksung Jo) 마은숙(Eunsook Ma)
• 간행물 정보: 『약학회지』제54권 제6호 (2010년), 466~473쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2010.12.31

영문 초록

A series of 3β-substituted 5-androstene-17β-carboxamides were synthesized from analogs of 3β-hydroxy-5-androstene-17β-carboxylic acid (1) with tert-butylamine, N,N-diethylamine and 3-aminopyridine and some compounds were epoxidized with mCPBA. A rat prostate testosterone 5α-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)-3β-carboxycarbonyloxy-5-androstene-17β-carboxamide (12) showed weak inhibitory activity (IC50: 2.4×10-7 M).

키워드

5α-reductase inhibitor prostate cancer benign prostatic hyperplasia 3β-substituted 5-androstene-17β-carboxamide