新型含吡啶基吡唑酰胺类化合物的合成与抗肿瘤活性  

Synthesis and biological activity of novel amides containing 1-(pyridin-2-yl) pyrazole derivatives

作　　者：蔡文玺 王润玲[1] 董卫莉[1] 刘艾林[2] 

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]中国医学科学院药物研究所,国家药物筛选中心,北京100050

出　　处：《天津医科大学学报》2016年第2期115-118,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特别资助项目(2014T70222),中国博士后科学基金面上项目(2011M500532)

摘　　要：目的:设计合成一系列新型的含吡啶基吡唑酰胺类化合物,并测试其生物活性。方法:以取代氨基苯甲酸和吡唑羧酸为起始原料,设计并合成了含吡啶基吡唑酰胺类化合物,测试化合物4a^4d对人肺癌A-549,人肝癌Bel7402和人肠癌HCT-8细胞的体外抗肿瘤活性。结果:合成了4个结构全新的含吡啶基吡唑酰胺类化合物,其结构通过1H NMR、红外光谱和元素分析进行了表征。体外抗肿瘤活性实验研究表明,化合物4d对Bel7402细胞株在浓度为5μg/mL时有较好的抑制活性,其他化合物也表现出一定的抑制活性。结论:化合物4d显示了较好的抑癌作用,值得进一步研究。Objective： To design and synthesize a series of novel amides containing 1-（pyridin-2-yl） pyrazole derivatives, and to evaluate their biological activities in vitro. Methods： A series of amides containing 1-（pyridin-2-yl） pyrazole derivatives were synthesized using substituted aminobenzoic acid and pyrazole carboxylic acid as starting materials and the biological activity of the title compounds 4a～4d were tested against A-549, Bel7402 and HCT-8 cell lines. Results： Four new types of amides containing 1-（pyridin-2-yl） pyrazole derivatives were synthesized and characterized by1 H NMR, IR and Elemental Analysis.The preliminary results indicated that the compound 4d showed inhibiting effects on Bel7402 cell line in vitro at the concentration of 5 μ g/mL, while showing no notable inhibiting activity against other cell 1ines. Conclusion： Compound 4d may have anticancer activity, and is worth further studying.

关 键 词：吡唑酰胺类 合成 抗肿瘤活性 

分 类 号：R9[医药卫生—药学]