含磺酰胺结构4-苯胺喹唑啉衍生物的合成与抗肿瘤活性评价

Synthesis and Antitumor Activities of 4-Anilinoquinazoline Derivatives Containing Sulfonamides

为获得抗肿瘤活性化合物以邻氨基苯甲腈和4-胺基苯磺酰胺为原料,通过2步反应合成了7个含磺酰胺结构的4-苯胺喹唑啉衍生物■,其结构经^(1)H NMR、^(13)C NMR和ESI-MS表征确证。利用MTT法考察了化合物■对Hep G2、A549、Hela、MCF-7细胞的抑制活性。结果表明,化合物■对四种细胞都具有抑制作用,以化合物■的作用最突出,对Hep G2、A549、MCF-7细胞的抑制强度分别是吉非替尼的5.4、1.5、3.0倍。

In order to obtain antitumor compounds,seven 4-anilinoquinazoline derivatives containing sulfonamide■ were synthesized from o-aminobenzonitrile and phenylsulfonamides through a two-step reaction process,and their structures were characterized by^(1)H NMR,^(13)C NMR and ESI-MS.the inhibitory effects of compounds■ on HepG2,A549,Hela and MCF-7 cells were investigated by MTT Assay.The results showed that compound■ had inhibitory effect on four kinds of cells,with compound■ being the most prominent.The inhibitory effect on HepG2,A549 and MCF-7 cells was 5.4,1.5 and 3.0 times that of Gefitinib,respectively.