Synthesis and biological evaluation of novel steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines

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• 作者：Li-Hua Huang^a ; ^b ; ^c ; Yong-Fei Zheng^a ; ^b ; Yong-Zheng Lu^c ; Chuan-Jun Song^c ; Yan-Guang Wang^a ; ^b ; Bin Yu^a ; ^b ; Hong-Min Liu^a ; ^b ; ^{liuhm@zzu.edu.cn}
• 关键词：Heterosteroids ; Steroidal[17 ; 16-d]triazolopyrimidines ; 1 ; 2 ; 4-Triazolo[1 ; 5-a]pyrimidines ; Anticancer activity
• 刊名：Steroids
• 出版年：2012
• 期刊代码：142_0039128x
• 类别：bio
• 出版时间：May, 2012
• 卷：77
• 期：6
• 页码：710-715
• 文件大小：378 K

摘要

The preparation of steroidal[17,16-d][1,2,4]triazolo[1,5-a]pyrimidines and their biological evaluation as potential anticancer agents are herein reported. These novel heterosteroids (2, 4) were prepared through the condensation reaction of 3-amino-1,2,4-triazole with 16-arylidene-17-ketosteroids (1, 3). All the synthesized compounds were evaluated for their anticancer activity in vitro against PC-3 (human prostatic carcinoma), MCF-7 (human breast carcinoma) and EC9706 (human esophageal carcinoma) cell lines. Among the screened compounds, 2i, 2n and 4f showed significant inhibitory activity against all the three human cell lines.