高等学校化学学报

高等学校化学学报 ›› 2001, Vol. 22 ›› Issue (6): 931.

• 研究论文 • 上一篇    下一篇

17α-羟化酶/C17,20-裂解酶(P45017α)抑制剂17-(取代吡唑、异噁唑基)雄烯衍生物的合成

茹呈杰1, 雷小平1, 凌仰之1, 张礼和1, Hundratta V.2, BrodieA. M. H.2   

  1. 1. 北京大学药学院, 北京 100083;
    2. 马里兰大学医学院药理和实验治疗系, 巴尔的摩MD 21201, 美国
  • 收稿日期:2000-08-21 出版日期:2001-06-24 发布日期:2001-06-24
  • 通讯作者: 凌仰之(1940年出生),男,教授,博士生导师,从事甾体化学与新药研究.E-mail:lingyz@public3.bta.net.cn E-mail:lingyz@public3.bta.net.cn
  • 基金资助:

    国家自然科学基金(批准号:39670855);美国NIH基金(批准号:CA27440)资助

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

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

  1. 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

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摘要： 在17-(3-吡唑基)和17-(5-异噁唑基)雄甾-4,16-二烯-3-酮的吡唑基的5-位和异噁唑基的3-位引入取代基,设计并合成了11个17-(取代的吡唑基、异噁唑基)雄烯衍生物,化合物的结构经1HNMR,IR,元素分析或质谱确证.

关键词: 细胞色素P45017&alpha, 酶, 良性前列腺增生, 前列腺癌, 抑制剂

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/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'-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 P45017α, Benign prostatic hypertrophy, Prostatic cancer, Inhibitors

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