D-ring substituted 1,2,3-triazolyl 20-keto pregnenanes as potential anticancer agents: Synthesis and biological evaluation

被引：133

作者：

Banday, Abid H. ^{[1
,2
]}

Shameem, Shameem A. ^{[1
]}

Gupta, B. D. ^{[2
]}

Kumar, H. M. Sampath ^{[2
]}

机构：

[1] Islamia Coll Sci & Commerce, Dept Chem, Srinagar 190009, Jammu & Kashmir, India

[2] Indian Inst Integrat Med, Synthet Chem Div, Jammu 180001, India

来源：

STEROIDS | 2010年 / 75卷 / 12期

关键词：

Triazoles; Pregnenolone; Click chemistry; INHIBITORS;

D O I：

10.1016/j.steroids.2010.02.015

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

A facile synthesis of 21-triazolyl derivatives of pregnenolone and their potential antitumour activity is reported. The scheme involves the transformation of the starting pregnenolone acetate into pregnenolone, conversion of pregnenolone to 21-bromo pregnenolone and finally the one-pot, two-step in situ conversion of the bromo derivative to the 21-triazolyl pregnenolone using the 'click chemistry' approach. These derivatives were screened for their anticancer activity against seven human cancer cell lines. The compounds especially 5a, 5b, 5c, Se, Sg and 5h exhibited significant anticancer activity with compound Se as the most active in this study. (C) 2010 Elsevier Inc. All rights reserved.

引用

页码：801 / 804

页数：4

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