17-Heterocyclic substituted androstene derivatives have been found to be potent inhibitors for human testicular microsomal 17α-hydroxylase/C17.20-layse, which have potential usage in the treatment of benign prostatic...17-Heterocyclic substituted androstene derivatives have been found to be potent inhibitors for human testicular microsomal 17α-hydroxylase/C17.20-layse, which have potential usage in the treatment of benign prostatic hypertrophy(BPH) and prostatic cancer. In order to further investigate their structure-activity relationships, seven new 17-[(2'-substituted)-4'-pyrimidyl]androstene derivatives were designed and synthesized. The structures of the compounds were confirmed by IR, ^1H NMR, elemental analysis or MS measurements. The results of the pharmacological activity tests showed that'compound 5 is a potent inhibitor for P45017α with IC50 225 nmol.L^-1.展开更多
文摘17-Heterocyclic substituted androstene derivatives have been found to be potent inhibitors for human testicular microsomal 17α-hydroxylase/C17.20-layse, which have potential usage in the treatment of benign prostatic hypertrophy(BPH) and prostatic cancer. In order to further investigate their structure-activity relationships, seven new 17-[(2'-substituted)-4'-pyrimidyl]androstene derivatives were designed and synthesized. The structures of the compounds were confirmed by IR, ^1H NMR, elemental analysis or MS measurements. The results of the pharmacological activity tests showed that'compound 5 is a potent inhibitor for P45017α with IC50 225 nmol.L^-1.
