新型邻苯磺酰氨基苯甲酰胺类化合物的合成与抗肿瘤活性  

Synthesis and antitumor activities of novel 2-phenylsulfonylamino benzamide derivatives

作　　者：郭翠翠[1,2] 刘文波[1] 董卫莉[1] 

机构地区：[1]天津医科大学药学院天津市临床药物关键技术重点实验室,天津300070 [2]中国人民武装警察部队医学院,天津300162

出　　处：《天津医科大学学报》2013年第4期275-278,共4页Journal of Tianjin Medical University

基　　金：国家自然科学基金青年基金资助项目(21102103);中国博士后科学基金面上项目(2011M500532)

摘　　要：目的:设计合成新型的邻苯磺酰氨基苯甲酰胺类化合物,并进行抗癌活性测试。方法:以取代苯胺和取代苯磺酰氯为起始原料,设计并合成了邻甲磺酰氨基苯甲酰胺类化合物,并采用MTT法测试了化合物8a^8d对人白血病细胞株HL-60,人胃癌BGC-823,人乳腺癌MDA和人子宫颈癌HeLa细胞株的体外抗肿瘤活性。结果:合成了4个邻甲磺酰氨基苯甲酰胺类化合物,均为新化合物,其结构经1H NMR和元素分析表征。体外抗肿瘤活性实验研究表明,化合物8a和8b对BGC-823细胞株在浓度为100μg/mL时有一定抑制率,其他化合物没有表现出明显的抑制活性。结论:化合物8a和8b显示了抑癌作用,值得进一步研究。Objective： To design and synthesize a series of novel 2-phenylsulfonylamino benzamide compounds, and to evaluate their antitumor activitie in vitro. Methods： A series of 2-phenylsulfonylamino benzamide compounds were synthesized using substitfited anilines and benzenesulfonyl chloride as starting materials and the antitumor activity of the title compounds 8a-8d against HL-60, BGC- 823, MDA and Hela cell lines were tested by MTT assay. Results： Four new types of 2-phenylsulfonylamino benzamide derivatives were synthesized and characterized by ^1H NMR and elemental analysis.The preliminary results indicated that the compound 8a and 8b showed inhibitory effects on BGC-823 cell line in vitro at the concentration of 100 μg/mL, while having no notable inhibitory activity against oth- er cell lines. Conclusion： Compound 8a and 8b proves to have anticancer activity, and is worth further study.

关 键 词：邻苯磺酰氨基苯甲酰胺 合成 抗肿瘤活性 

分 类 号：R9[医药卫生—药学]