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

页码：413 / 415

页数：3

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