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

Chemical Research in Chinese Universities(2001)

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摘要
 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.
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inhibitors
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