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以2-氨基-5-取代苯并噻唑为原料,经水解、缩合反应合成了系列全新结构的5-取代-2-(吡啶基)苯并噻唑类化合物。以Bcap-37、HCT-15、HepG2肿瘤细胞为靶细胞,五氟尿嘧啶(5-FU)为阳性对照,采用MTT法测试化合物的体外活性。结果显示,多数化合物对肿瘤细胞有一定程度的抑制作用,而对正常细胞293T、L02无明显作用。优选出的化合物lc对HCT-15、2e对HepG2、1i对Bcap-37和HepG2细胞具有较好活性,IC50值分别为41.59、38.65、46.63和23.51μmol.L 1。在此基础上,初步讨论了该类化合物的构效关系。
A series of novel 5-substituted-2- (pyridyl) benzothiazoles were synthesized by hydrolysis and condensation reaction using 2-amino-5-substituted benzothiazoles as starting materials. Bcap-37, HCT-15, HepG2 tumor cells as target cells, and 5-fluorouracil (5-FU) as a positive control, the compounds were tested for their in vitro activity by MTT assay. The results show that most compounds have a certain degree of inhibition of tumor cells, while normal cells 293T, L02 no significant effect. The preferred compound lc has good activity on HepG2,1i against Bcap-37 and HepG2 cells with IC50 values of 41.59, 38.65, 46.63 and 23.51 μmol.L 1 for HCT-15 and 2e respectively. On this basis, the structure-activity relationship of these compounds is discussed preliminarily.