苯乙烯喹啉衍生物的合成及抗癌活性研究

Syntheses and Antitumor Activities Evaluation of Styryl Quinoline Derivatives

摘要:

以取代的苯胺和反式丁烯醛为原料，在盐酸中反应得到4个2 -甲基喹啉衍生物，所得产物再与芳香醛在冰醋酸中回流反应合成了10个苯乙烯喹啉衍生物，收率为64% ~ 78%。所得化合物的结构经1HNMR、MS、IR表征确认，并采用MTT法进行初步体外抗肿瘤活性筛选。结果表明，化合物Ⅱc对A 549和HCT 116细胞均有较高的抑制活性，IC50值分别为9.77和9.66 μmol/L，化合物Ⅱd对HCT 116细胞有较高的抑制活性，IC50值为9.80 μmol/L。

Abstract:

Ten styrylquinoline derivatives were prepared from anilines and aromatic aldehydes in two steps. Firstly, four 2 -methylquinolines have been synthesized from anilines and (E)-2-butenal using hydrochloric acid as catalyst. Then styrylquinolines were obtained with 64% ~ 78% yield by refluxing 2-methylquinolines and aromatic aldehydes in glacial acetic acid. The structures of all synthesized compounds were confirmed by 1HNMR, MS and IR. The antitumor activity of these compounds against A 549 and HCT 116 cell lines was evaluated by MTT assay in vitro. The results showed that compounds Ⅱc exhibited high activity against A 549 and HCT 116 cell lines with IC50 value of 9.77 and 9.66 μmol·L-1, respectively, and compounds Ⅱd exhibited high activity against HCT 116 cell lines with IC50 value of 9.80 μmol·L-1 .