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%.