新型N-[2-(取代苯并噻唑-2-氨基甲酰基)苯基]取代氟基苯甲酰胺的合成及其抗癌活性

Synthesis and Anticancer Activities of Novel N-[2-(substituted benzothiazol-2-carbamoyl)phenyl] substituted-fluoro-benzamides

2,4-二氟苯甲酸或2-氟苯甲酸与二氯亚砜经酰氯化反应,再与邻氨基苯甲酸反应后在醋酸酐中闭环,最后与取代苯并噻唑胺反应合成了9个新型的N-[2-(取代苯并噻唑-2-氨基甲酰基)苯基]取代氟基苯甲酰胺(6a～6i),其结构经1H NMR,13C NMR,IR和元素分析表征。采用MTT法对6a～6i进行抑制PC3癌细胞体外活性测试,结果表明6a～6i具有不同程度的抑制PC3癌细胞活性,其中10μmol.L-16b对PC3的抑制率为69.9%。

Nine novel N-[ 2-（ substituted benzothiazol-2-carbamoyl）phenyl] substituted-fluoro- benzamides （6a - 6i） were sythesized by the acyl chlorination of 2-fluorobenzoic acid or 2,4-difluorobenzoic acid with thionyl chloride, then coupled with 2-aminobenzoic acid, cyclized in the presence of acetic anhydride, in the end coupled with substituted benzo[ d] thiazol-2-amine. The structures were characterized by 1H NMR, 13C NMR, IR and elemental analysis. Preliminary bioassay tests indicated that 6a - 6i exhibited antitumor activities to PC3 cells in vitro by MTT method. The antiproliferation activity of 6b（ 10 μmol·L^-1） to PC3 ceils was 69.9%.