摘要
以19-羟基雄甾-4-烯-3,17-二酮(1)为先导物,经4β,5β-环氧化得8,然后4-位,引入取代基如羟基、氯、溴及乙酰硫基(2、3、4及5)。并用HPLC法测定其对人胎盘微粒体睾丸素A环芳香化酶的相对抑制活性,结果表明3活性较强。
The 4-substituted derivatives of 19-bydroxy-4-androstene -3, 17-dione (1) as inhibitors of testosterone A-ring aromatase were synthesized from 1via 4 β, 5β-epoxy-19- hydroxyandrostane -3, 17-dione (8). 4,19-Dihydroxy-4-and-rostene-3, 17-dione (2) and its 4-chloro analong (3) could effectively inhibit thearomatization of 4-androstene-3, 17-dione by human placenta aromatase.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1989年第8期347-348,381,共3页
Chinese Journal of Pharmaceuticals
基金
国家自然科学基金资助课题
关键词
雄甾烯二酮
合成
抑制剂
芳香化酶
inhibitor, testosterone A-ring aromatase, 4-substituted 19-hydroxy-4-androstene-3. 17-dione
