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应用生物电子等排原理,设计并合成了两类共24个含芳基哌嗪的苯并噻唑衍生物。采用MTT法评价了化合物对4种癌细胞和2种正常细胞的抗增殖作用。结果表明,大部分化合物对于癌细胞的增殖都有一定程度的抑制作用,其中化合物II2、II3、II6和II7对HepG2和HeLa229细胞具有较强的抗增殖作用,其IC50值分别为1.6～4.5μmol.L 1和2.5～5.3μmol.L 1;苯环对位引入氰基的化合物(Ι4、Ι8、Ι12、II4、II8、II12)对AsPC-1细胞具有较好的抗增殖作用,IC50值为5.2～11.3μmol.L 1,在此基础上初步探讨了此类化合物的构效关系。
A total of 24 benzothiazole derivatives containing aryl piperazines were designed and synthesized using bioisosterism principle. The anti-proliferative effects of the compounds on four kinds of cancer cells and two kinds of normal cells were evaluated by MTT method. The results showed that most of the compounds inhibited the proliferation of HepG2 and HeLa229 cells to a certain extent. The compounds of compounds II2, II3, II6 and II7 had strong antiproliferative effects on HepG2 and HeLa229 cells with IC50 values of 1.6-4.5 μmol .L 1 and 2.5 ~ 5.3μmol.L 1; the compounds (I4, I8, I12, II4, II8, and II12) with the cyano group introduced into the para position of the benzene ring had a good antiproliferative effect on AsPC- 5.2 ~ 11.3μmol.L 1, on the basis of this preliminary study of the structure-activity relationship of these compounds.