Syntheses of Some 17-Heterocyclic Substituted Androstene Derivatives as Inhibitors of Human 17α-Hydroxylase/C17,20-layse(P45017α)

Chem. J. Chinese Universities ›› 2001, Vol. 22 ›› Issue (6): 931.

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Syntheses of Some 17-Heterocyclic Substituted Androstene Derivatives as Inhibitors of Human 17α-Hydroxylase/C_17,20-layse(P450_17α)

RU Cheng-Jie¹, LEI Xiao-Ping¹, LING Yang-Zhi¹, ZHANG Li-He¹, Hundratta-V.², BrodieA. M. H.²

1. School of Pharmaceutical Sciences, Peking University, Beijing 100083, China;
2. Department of Pharmacology & Experimental Therapeutics, School of Medicine, University of Maryland, Baltimore, MD 21201, USA

Received:2000-08-21 Online:2001-06-24 Published:2001-06-24

Abstract

Abstract: 172(3'-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 MSmeasurements. Their pharmacological activities are under investigation.

Key words: Cytochrome P450_17α, Benign prostatic hypertrophy, Prostatic cancer, Inhibitors

CLC Number:

O629

TrendMD:

RU Cheng-Jie, LEI Xiao-Ping, LING Yang-Zhi, ZHANG Li-He, Hundratta-V. , BrodieA. M. H. . Syntheses of Some 17-Heterocyclic Substituted Androstene Derivatives as Inhibitors of Human 17α-Hydroxylase/C_17,20-layse(P450_17α)[J]. Chem. J. Chinese Universities, 2001, 22(6): 931.

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Syntheses of Some 17-Heterocyclic Substituted Androstene Derivatives as Inhibitors of Human 17α-Hydroxylase/C_17,20-layse(P450_17α)

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