论文部分内容阅读
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。
Thiazole ring and hydrazone bond structure have some biological activity, the active structure splicing method, the thiazole ring and hydrazone bond, designed and synthesized 16 2-aryl-hydrazone thiazoles and MTT method for the target compound In vitro antitumor activity screening. The test results show that the new compounds have certain anti-proliferative activity on breast cancer cell lines (MDA-MB-231, MDA-MB-468, MCF-7) Among them, the anti-proliferative activity of N- (2-pyridyl) formaldehyde-2- (4-phenyl) thiazolyl hydrazone was the best. The IC50 values were 0.21 ± 0.11, 0.18 ± 0.10, 0.17 ± 0.08, μmol / L, and the compound has certain anti-proliferative activity on other tumor cells, and the biological activity of the compound is 10 times or more than that of the breast cancer cell lines, indicating that the compound has good biological activity and selectivity for breast cancer cells , And the side effects of small, worth as a leading compound against breast cancer for further study.