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苯乙烯喹啉衍生物的合成及抗癌活性 被引量:1

Syntheses of Styrylquinoline Derivatives and Evaluation of Their Antitumor Activities
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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9.66μmol/L,化合物Ⅱd对HCT 116细胞有较高的抑制活性,IC50值为9.80μmol/L。 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 in yields ranging between 64% ~78% by refluxing 2-methylquinolines and aromatic aldehydes in glacial acetic acid. The structures of all the synthesized compounds were confirmed by1 HNMR,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 show that compounds Ⅱc exhibits high activity against A 549 and HCT 116 cell lines with IC50 value of9. 77 and 9. 66 μmol/L,respectively,and compounds Ⅱd exhibits high activity against HCT 116 cell lines with IC50 value of 9. 80 μmol/L.
出处 《精细化工》 EI CAS CSCD 北大核心 2015年第10期1132-1136,共5页 Fine Chemicals
关键词 喹啉 苯乙烯基 2-甲基喹啉 抗癌活性 医药与日化原料 quinoline styryl 2-methylquinoline antitumor activities drug and cosmetic materials
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