N-(2-(取代苯并噻唑-2-氨基甲酰基)-取代苯基)-4-氟苯甲酰胺衍生物的合成及生物活性  

Synthesis and biological activity of N-(2-(substituted benzothiazol-2-carbamoyl) substituted phenyl-4-fluoro benzamide derivatives

作　　者：薛伟[1] 郑玉国[1,2] 熊壮[1] 祁慧雪[1] 范会涛[1] 何勇[1] 卢平[1] 李海畅[1] 

机构地区：[1]贵州大学精细化工研究开发中心,教育部绿色农药与农业生物工程重点实验室,贵州贵阳550025 [2]兴义民族师范学院化学生物系,贵州兴义562400

出　　处：《分子科学学报》2012年第3期207-213,共7页Journal of Molecular Science

基　　金：国家自然科学基金资助项目(21062005);贵州省十一五农业攻关资助项目(20083061)

摘　　要：以对氟苯甲酸和取代邻氨基苯甲酸为起始原料,设计并合成11个含氟基苯并噻唑基邻甲酰氨基苯甲酰胺类化合物,其结构经1 H NMR、13C NMR、IR及元素分析确证.初步生物活性测试结果表明,在500mg/L浓度下部分化合物对烟草花叶病毒(TMV)有一定抑制作用.采用MTT法进行化合物抑制PC3及Bcap-37癌细胞体外活性测试,结果表明所合成的化合物具有不同程度的抑制PC3和Bcap-37癌细胞活性,其中化合物4d在10μmol.L-1浓度下对PC3和及Bcap-37的抑制率分别为73.2%和68.1%.Eleven novel diamides compounds containing fluorine and benzothiazole moieties were synthesized. Their structures were characterized by ^1H NMR, ^13 C NMR, IR and elemental analyses. The preliminary bioassay shows that some compounds exhibited certain antiviral activities and antitumor activity to PC3 and Bcap37 cells in vitro by MTT method. The antiproliferation activity of compound 4d to PC3 and Beap37 cells at the concentration of 10μmol.L^-1 was 73.2 % and 68. 1%.

关 键 词：双酰胺 苯并噻唑 氟 生物活性 合成 

分 类 号：O626[理学—有机化学]