磷酰胺类化合物的合成及抗K562细胞活性研究

Synthesis and Anti-K562 Cell Activity of Phosphoramide Compounds

目的合成并评价磷酰胺类化合物体外对白血病细胞株 K562 生物活性的抑制作用。方法以芳氨基为药效基团,羟脯氨酸为载体设计目标物,通过几步亲核取代反应合成一系列新化合物,并表征其结构。MTT 法测定它们对人慢性髓性白血病细胞株 K562 细胞的抑制作用。结果发现了 10 个新化合物有一定的生物活性。结论发现了一类新的具有一定抗肿瘤活性的磷酰胺类先导化合物。

OBJECTIVE To synthesis and evaluate a series of novel phosphoramide compounds, and to evaluate their in vitro inhibitory activity of leukemia in K562 cells. METHODS The target compounds were designed by using aryl amino as active group while hydroxyproline as carrier moiety, they were synthesized by several nucleophilic substitution reaction, whose structures were characterized, the inhibitory effects of which on human chronic myeloid leukemia cell line K562 were determined by MTT assay. RESULTS Ten new compounds exhibited certain biological activity against K562 cells. CONCLUSION A new class of phosphoramide leading compounds with certain anti-tumor activity is found.