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以2-羟基-3-甲氧基苯甲醛为原料,经13步反应合成了26个那可丁衍生物。以HL-60细胞为靶细胞,采用MTT法进行了初步的体外抗肿瘤活性研究。结果表明,大多数化合物对HL-60细胞株显示出较好的抑制活性和对微管聚合的抑制作用。优选出的化合物31对HL-60细胞株以及微管聚合的抑制活性是那可丁的3倍并诱导HL-60细胞在G2/M期累积,这为那可丁及其衍生物的抗肿瘤活性构效关系的研究打下了基础,值得进一步研究。
Using 2-hydroxy-3-methoxybenzaldehyde as raw material, 26 nakatine derivatives were synthesized in 13 steps. Using HL-60 cells as target cells, MTT assay was used to study the antitumor activity in vitro. The results showed that most of the compounds showed good inhibitory activity on HL-60 cell lines and inhibition of microtubule polymerization. The preferred compound 31 has 3-fold more potent inhibitory activity on HL-60 cell line and microtubule polymerization than nadine and induces the accumulation of HL-60 cells at G2 / M phase, which is an antitumor effect of nocodine and its derivatives The study of the activity-activity-activity relationship lays the foundation and deserves further study.