5H-噻唑并[3,2-a]嘧啶类化合物的合成及抗肿瘤活性研究  

Synthesis and Antitumor Activities of 5H-thiazolo [3,2-a]pyrimidine Derivatives

作　　者：王彩虹[1] 贾云宏[1] 蔡东[1] 

机构地区：[1]辽宁医学院药学院,锦州121001

出　　处：《化学通报》2014年第2期174-177,共4页Chemistry

摘　　要：以芳醛、硫脲等为起始原料,通过Biginelli反应合成二氢嘧啶类化合物,再与取代的溴代苯乙酮发生Hantzsch环合反应得到目标化合物。所有化合物的结构都经过1H NMR、13C NMR、IR和HRMS表征确认。在此基础上以MCF-7、A549和HT-29为靶细胞,顺铂为阳性对照物,采用噻唑蓝检测法进行初步体外抗肿瘤活性筛选。结果表明,化合物3c对HT-29的体外抗肿瘤活性与对照药物相当,值得进一步研究。The target compounds were synthesized with Hantzsch condensation of dihydropyrimidines, which was obtained by Biginelli reaction between aromatic aldehydes and thiourea, with substituted 2-bromo-1- phenylethanone. The structures of products were characterized by IH NMR, 13C NMR, IR, and HRMS. The antitumor activities of as-synthesized compounds were evaluated against MCF-7, A549 and HT-29 in vitro by MTT assay （ cisplatin as a control）. The results showed that antitumor activity of compound 3c on HT-29 cells were similar to control drug. So it is worthy to study further.

关 键 词：噻唑并[3 2-a]嘧啶 合成 抗肿瘤活性 

分 类 号：O626[理学—有机化学]