含氮芥和亲脂基团的聚磷酸酯的合成及其抗肿瘤活性的初步研究

本文通过3-烷氧基1,2-丙二醇与N,N'-双(2-氯乙基)二氯磷酰胺的缩合反应,制得11种新的含氮芥和亲脂基团的聚磷酸酯.用核磁、红外光谱以及元素分析确定了聚合物的结构.部分聚合物抗肿瘤初步试验结果表明.这类聚磷酸酯对小鼠肉瘤180有一定的抑制作用.在本研究中还改进了3-烷氧基-1,2-丙二醇的合成方法.

Studies on the Synthesis and Antitumor Activity of Polyphosphates Containing Both Nitrogen Mustard and Lipophilic Groups

11 New poly phosphates containing both nitrogen mustard and lipophilic groups were synthesized by the polycondensation of N,N'-bis(2-chloroethyl)phosphoramido dichloride with 3-alkoxy-1, 2-propanediol in bezene and in the presence of triethylamine.The polyphosphates were structurally characterized by ¹H NMR, IRspectra and elemental analysis.All of the polymers obtained are insoluble in water, but soluble in common organic solvents.The antitumor activity of some of these polymers were tested against Sarcoma 180 in mice.Polymer Ⅲe exhibits an inhibition ratio of 54.5%.