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学科主题: 药学
题名:
Novel P450(17 alpha) inhibitors: 17-(2 ′-oxazolyl)- and 17-(2 ′-thiazolyl)-androstene derivatives
作者: Zhu, N; Ling, YZ; Lei, XP; Handratta, V; Brodie, AMH
关键词: P450(17 alpha) inhibitors ; 17-(2 &prime ; -oxazolyl)-androstenes ; 17-(2 &prime ; -thiazolyl)-androstenes ; prostatic cancer
刊名: STEROIDS
发表日期: 2003-09-01
DOI: 10.1016/S0039-128X(03)00082-5
卷: 68, 期:7-8, 页:603-611
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Endocrinology & Metabolism
研究领域[WOS]: Biochemistry & Molecular Biology ; Endocrinology & Metabolism
关键词[WOS]: STEROIDAL INHIBITORS ; KETOCONAZOLE THERAPY ; POTENTIAL AGENTS ; PROSTATIC-CANCER
英文摘要:

Twelve 17-(2′-oxazolyl)- and 17-(2′-thiazolyl)-androsta-5,16-diene derivatives were designed and synthesized from 3beta-acetoxy-pregna-5,16-dien-20-one (1b) as inhibitors of 17alpha-hydroxylase-C-17,C-20-lyase (P450(17alpha)). Potent inhibitors of this enzyme could be of value as treatment of prostate cancer. Two substituents (methyl and phenyl) were introduced either at their 4′- or 5′-position in order to investigate their structure-activity relationship. Due to the 16,17-double bond, 17-thiazoles were generally obtained in low yield. The pharmacological results showed that the compounds containing 17-(2′-oxazolyl) (14c) and 17-(2′-thiazolyl) (8c) (41.5%) demonstrated reasonable inhibition against P45017a. Their 3-acetate (13c and 7c) were less potent than their 3-OH counterparts. The introduction of a phenyl or methyl group generally decreased inhibitory activity. Surprisingly, 17-(5′-methyl-2′-thiazolyl) (12a) was the most potent compound in this series and was almost as potent as L-39, which has good antitumor activity. (C) 2003 Elsevier Inc. All rights reserved.

语种: 英语
WOS记录号: WOS:000185377000005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59745
Appears in Collections:北京大学药学院_药物化学系_期刊论文

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作者单位: 1.Univ Maryland, Sch Med, Dept Pharmacol & Expt Therapeut, Baltimore, MD 21201 USA
2.Peking Univ, Ctr Hlth, Sch Pharmaceut Sci, Dept Med Chem, Beijing 100083, Peoples R China

Recommended Citation:
Zhu, N,Ling, YZ,Lei, XP,et al. Novel P450(17 alpha) inhibitors: 17-(2 ′-oxazolyl)- and 17-(2 ′-thiazolyl)-androstene derivatives[J]. STEROIDS,2003,68(7-8):603-611.
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