新型含氮杂环类他米巴罗汀类似物的合成及活性研究

Design,synthesis and activities of novel tamibarotene analogues containing nitrogen heterocyclic ring

目的:设计合成3个新型含氮杂环类他米巴罗汀类似物,对活性进行研究。方法:以2,5-二甲基-2,5-己二醇和草酸二乙酯为起始原料,经过9步反应合成目标化合物。采用了MTT法测试了3个化合物对HL-60细胞和NB4细胞的抑制作用。结果与结论:目标化合物结构经1H-NMR,ESI-MS及元素分析确证。3个化合物对于HL-60细胞和NB4细胞均有一定的抑制作用。

Objective： To design, synthesize and evaluate three novel tamibarotene analogues containing nitrogen heterocyclic ring. Methods： Target compounds were synthesized through 8 steps using 2,5-dimethyl-2,5- hexanediol and diethyl oxalate as starting materials. In vitro antitumor bioactivities against HL-60 cells and NB4 cells were evaluated by a MTT assay method. Results and Conclusion： Their structures were identified by 1^H-NMR, MS and elemental analysis. Three compounds had inhibitory effects on HL-60 cells and NB4 cells