2-芳醛腙噻唑类化合物的合成及其抗肿瘤活性

噻唑环和腙键结构均具有一定的生物活性,采用活性结构拼接法,将噻唑环与腙键相结合,设计并合成了16个2-芳醛腙噻唑类化合物,并采用MTT法对目标化合物进行体外抗肿瘤活性筛选。测试结果表明,该类新化合物对乳腺癌细胞株(MDA-MB-231、MDA-MB-468、MCF-7)具有一定的抗增殖活性。其中,N-(2-吡啶)甲醛-2-(4-苯基)噻唑腙的抗增殖活性最好,其IC50值分别为(0.21±0.11)、(0.18±0.10)、(0.17±0.08)μmol/L;而该化合物对其他肿瘤细胞亦具有一定的抗增殖活性,且相对乳腺癌细胞株的生物活性均在10倍及以上,说明其对乳腺癌细胞具有较好的生物活性和选择性,且毒副作用小,值得作为抗乳腺癌先导化合物进行进一步研究。

Synthesis and Antitumor Activity of 2-Thiazolylhydrazyne Scaffold Derivatives

Thiazole ring and hydrazone structure have certain biological activity.In this work,we applied the active structure-linking method,which is combining thiazole and hydrazone,and have designed and synthesized a series of novel 2-thiazolylhydrazyne scaffold derivatives.The structures were confirmed by 1HNMR and elemental analysis.These compounds were evaluated for antibreast cancer activity on MDA-MB-231,MDA-MB-468,MCF-7 cells by MTT method in vitro.The test results show that this kind of new compounds has antiproliferative activity.And N-(4-phenyl-thiazole-2-yl)-2-pyridine hydrazone exhibited better antiproliferative activity against MDA-MB-231,M DA-MB-468,MCF-7 breast cells with the C50 value of (0.21 ± 0.11),(0.18 ± 0.10),(0.17±0.08) μmol/L,respectively.This compound also has certain antiproliferative activity against the other tumor cells (PANC-1,Hela,MKN45,SKOV3,Karpas299,Ramos).And the relate selectivity of compound against MDA-MB-231 cell are more than 10 times.The results show that it has good biological activity and selectivity against breast cancer cells with low side effects.So above compound is worth as lead compound of breast cancer for further research.