Syntheses of some 17-heterocyclic substituted androstene derivatives as inhibitors of human 17-hydroxylase/C17,20-layse (P45017)

17-(3 prime -Pyrazolyl) and 17-(5 prime -isoxazolyl)androsta-4,16-dien-3-one have been found to be potent inhibitors for human testicular microsomal 17??-hydroxylase/C17,20-layse, which showed potential usage in the treatment of benign prostatic hypertrophy (BPH) and prostatic cancer. In order to further investigate their structure-activity relationship, some substituents were introduced at the 5 prime -position of pyrazole and 3 prime -position of isoxazole, and eleven derivatives were obtained. The structures of the compounds were confirmed by IR, 1H NMR, elemental analysis or MS measurements. Their pharmacological activities are under investigation.SCI(E)EI中文核心期刊要目总览(PKU)中国科学引文数据库(CSCD)06931-9352