水杨醛-ɑ-氨基膦酸酯衍生物的合成 及抗肿瘤活性

Synthesis and Antitumor activities of salicylaldehyde-ɑ-aminophosphate derivatives

摘要:

以ɑ-氨基膦酸酯和邻羟基苯甲醛为原料，经缩合反应（微波辅助）、NaBH4还原,合成了10个结构新颖的水杨醛-ɑ-氨基膦酸酯衍生物，所有目标化合物的结构均经过IR，1H-NMR，13C-NMR和HRMS确认。优化微波合成条件为：25℃时，功率600W，反应25min，产率达到86.3%。利用MTT法测定了目标化合物的抗肿瘤活性,结果显示：目标化合物对用于测试的三种肿瘤细胞：人急性髓系白血病细胞（KGla）、人肝癌细胞（HepG2）、宫颈癌细胞（Hela）均有一定的抑制作用，其中3E、3F对HepG2表现出较好的增殖抑制作用。

Abstract:

Ten novel salicylaldehyde-ɑ-aminophosphonate derivatives were synthesized through the condensation reaction (microwaved-assisted method) and NaBH4 as the reduction agent, using ɑ-aminophosphate derivatives and o-hydroxybenzaldehydes as the starting materials. All of the target compounds were characterized by IR, 1H-NMR, 13C NMR and HRMS. The optimum conditions were as following: microwaved reaction at 25℃,600W for 25min. The antitumor activity of the target compounds was determined by MTT method. The results showed that the target compounds had inhibitory effects against three kinds of tumor cells: human acute myeloid leukemia cells (KGla), human hepatoma cells (HepG2), cervical cancer cells (Hela). Among the ten compounds, 3E, 3F showed a good inhibitory activity against HepG2.