Steroidal[17,16-d] pyrimidines derived from dehydroepiandrosterone: A convenient synthesis, antiproliferation activity, structure-activity relationships, and role of heterocyclic moiety
文献类型： 外文期刊
第一作者： Ke, Shaoyong
作者： Ke, Shaoyong;Shi, Liqiao;Zhang, Zhigang;Yang, Ziwen
作者机构：
期刊名称：SCIENTIFIC REPORTS （ 影响因子：4.379； 五年影响因子：5.133 ）
ISSN： 2045-2322
年卷期： 2017 年 7 卷
页码：
收录情况： SCI
摘要： A series of steroidal[17,16-d] pyrimidines derived from dehydroepiandrosterone were designed and prepared by a convenient heterocyclization reaction. The in vitro anticancer activities for these obtained compounds were evaluated against human cancer cell lines (HepG2, Huh-7, and SGC-7901), which demonstrated that some of these heterocyclic pyrimidine derivatives exhibited significantly good cytotoxic activities against all tested cell lines compared with 5-fluorouracil (5-FU), especially, compound 3b exhibited high potential growth inhibitory activities against all tested cell lines with the IC50 values of 5.41 +/- 1.34, 5.65 +/- 1.02 and 10.64 +/- 1.49 mu M, respectively, which might be used as promising lead scaffold for discovery of novel anticancer agents.
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