17α-羟化酶/C_(17,20)-裂解酶(P450_(17α))抑制剂17-(取代吡唑、异噁唑基)雄烯衍生物的合成

Syntheses of Some 17-Heterocyclic Substituted Androstene Derivatives as Inhibitors of Human 17α-Hydroxylase/C_(17,20)-layse(P450_(17α))

在 1 7-( 3 -吡唑基 )和 1 7-( 5 -异噁唑基 )雄甾 -4 ,1 6-二烯 -3 -酮的吡唑基的 5 -位和异唑基的 3 -位引入取代基 ,设计并合成了 1 1个 1 7-(取代的吡唑基、异唑基 )雄烯衍生物 ,化合物的结构经 1H NMR,IR。

 Pyrazolyl) and 17 (5 isoxazolyl)androsta 4,16 dien 3 one have been found to be potent inhibitors for human testicular microsomal 17α hydroxylase/C 17,20 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 position of pyrazole and 3 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.