新型双酰胺衍生物的合成及抗癌活性

Synthesis and Antitumor Activity of Novel Bisamide Compounds

以取代苯甲酸为起始原料,设计合成了10个含苯并噻唑基双酰胺类化合物,其结构经1HNMR、13CNMR、IR及元素分析确证。采用MTT法进行化合物抑制PC3、BGC-823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地抑制癌细胞活性,其中化合物N-[2-(6-甲基苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-4-氯苯甲酰胺(Ⅳa)和N-[2-(4-甲基苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-2-甲基苯甲酰胺(Ⅳe)在10μmol/L浓度下对PC3的抑制率为70.8%和68.4%,N-[2-(苯并噻唑-2-氨基甲酰基)-4-甲基苯基]-2-甲基苯甲酰胺(Ⅳd)在10μmol/L浓度下对BGC-823的抑制率为65.9%。

Ten novel bisamide compounds containing benzothiazole unit were synthesized from the starting material of substituted benzoic acid. Their structures were characterized by means of 1HNMR, 13CNMR, IR and elemental analyses. Preliminary bioassay indicates that some compounds posed antitumor activity to PC3 and BGC -823 cells in vitro by MTT method. The antiproliferation activity of compound N-[ 2- （6-methylbenzothiazole-2-ylcarbamoyl） -4-methylphenyl ] -4-chlorobenzenecarboxamide （ Ⅳa ） and N-[ 2-（ 4-methylbenzothiazole-2-ylcarbamoyl ）-4-methylphenyl ]-2-methylbenzene earboxamide（Ive） to PC3 cells at the concentration of 10 μmol/L was 70. 8% and 68.4% respectively. And the antiproliferation activity of compound N-[ 2-（ benzothiazole-2-ylcarbamoyl ）-4- methylphenyl]-2-methylbenzenecarboxamide（ Ⅳ d） to BGC -823 cells at the concentration of 10 μmol/L was 65.9%.