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

摘要

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10μ mol·L-1 6b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-difluoro-benzoic 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 antiprolif-eration activity of 6b( 10 μmnol · L-1) to PC3 cells was 69. 9%.