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为寻找抗白血病活性化合物,本研究以对甲基苯乙酮、芳香醛和芳香胺为原料,借助Mannich反应一锅法合成了33个曼尼希碱,其结构经1H NMR、IR、MS确证;体外活性测试结果表明,在1×10~(-4) mol·L~(-1)浓度下,所有化合物对P338肿瘤细胞生长显示抑制作用,在测试浓度为1×10~(-8) mol·L~(-1)时,化合物TM33抑制活性最好,其抑制率依然高达60.3%、半数抑制浓度IC_(50)低至0.45 nmol·L~(-1)。本研究为新型抗白血病药物的研发提供了新的分子类型。
In order to find an active compound against leukemia, 33 Mannich bases were synthesized by one-pot Mannich reaction using p-methylacetophenone, aromatic aldehyde and aromatic amine as raw materials. Their structures were confirmed by 1H NMR, IR and MS The results of in vitro activity test showed that all the compounds showed inhibitory effects on the growth of P338 tumor cells under the concentration of 1 × 10 -4 mol·L -1. The inhibitory rate of TM33 was still up to 60.3% and the IC50 of 50 was as low as 0.45 nmol·L -1. This study provides a new molecular type for the development of new anti-leukemia drugs.