5H-噻唑并[3,2-a]嘧啶类化合物的合成及抗肿瘤活性研究

• 作 者: 王彩虹 贾云宏 蔡东
• 机 构: 辽宁医学院药学院,
• 出 处: 化学通报
• 发表日期: 2014年02期
• 关键词: 体外抗肿瘤活性 嘧啶类化合物 目标化合物 合成 对照药物 苯乙酮 芳醛 溴代 抗肿瘤活性 环合反应

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。

Starting from aromatic aldehydes and thioureas, the dihydropyrimidines were synthesized by Biginelli reaction and then Hantzsch cyclization reaction was carried out with the substituted bromoacetophenones to give the target compounds. The structures of all compounds were confirmed by 1H NMR, 13C NMR, IR and HRMS characterization. On this basis, MCF-7, A549 and HT-29 as target cells, cisplatin as a positive control, using thiazolyl blue assay for preliminary in vitro anti-tumor activity screening. The results showed that the antitumor activity of compound 3c against HT-29 in vitro was comparable to that of the control drug, which deserved further study.