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

作　　者：梁光平 文露滴 梁光焰 王道平[2] 邱佳[1] 万路平 杨俊 LIANG Guang-ping;WEN Lu-di;LIANG Guang-yan;WANG Dao-ping;QIU Jia;WAN Lu-ping;YANG Jun(Department of Pharmacy,Zunyi Medical and Pharmaceutical College,Zunyi 563006,China;The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550014,China)

机构地区：[1]遵义医药高等专科学校药学系,贵州遵义563006 [2]贵州省中国科学院天然产物化学重点实验室,贵州贵阳550014

出　　处：《精细化工中间体》2022年第1期28-31,38,共5页Fine Chemical Intermediates

基　　金：贵州省科学技术基金资助项目(黔科合基础[2019]1356号);遵义医药高等专科学校博士科研启动项目(遵医专科合BS2018001号)。

摘　　要：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.

关 键 词：喹唑啉 表皮生长因子 合成 抗肿瘤 

分 类 号：R914.5[医药卫生—药物化学]