Synthesis and cytotoxic activity of novel steroidal derivatives containing a [1,2,4]triazolo[1,5-a]pyrimidine ring

被引：20
|
作者：
Fan, Ning-Juan [1 ]
Li, Yuan-feng [1 ]
Liang, Shuang [1 ]
Tang, Jiang-Jiang [2 ]
机构：
[1] Northwest A&F Univ, Coll Life Sci, Biochem & Mol Biol Res Platform, Yangling 712100, Shaanxi, Peoples R China
[2] Northwest A&F Univ, Coll Sci, Shaanxi Engn Ctr Bioresource Chem & Sustainable U, Yangling 712100, Shaanxi, Peoples R China
来源：
JOURNAL OF CHEMICAL RESEARCH | 2017年 / 07期
基金：
中国国家自然科学基金;
关键词：
progesterone; Claisen condensation; antiproliferative activity; 1,2,4-triazolo[1,5-a]pyrimidines;
D O I：
10.3184/174751917X14967701767003
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The synthesis of steroidal derivatives containing [1,2,4] triazolo[1,5-a] pyrimidine derived from progesterone is described. The Claisen condensations of Delta(1,4)-pregnadien-3,20-dione and 4-chloro-.1,4-pregnadien-3,20-dione with dimethyl oxalate afforded 21-methoxalylpregn1,4-diene-3,20-dione and 4-chloro-21-methoxalylpregn-1,4-diene-3,20-dione, respectively. Furthermore, the reactions of these compounds with 3-amino-1,2,4-triazole yielded the corresponding [1,2,4] triazolo[1,5-a] pyrimidine derivatives. The newly synthesised compounds were evaluated in vitro by means of sulforhodamine B assays for antiproliferative activity against HeLa and MCF-7 cells.
引用
收藏
页码：413 / 415
页数：3
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