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聚乙撑亚胺在体内、体外均显示一定的抗癌活性,但由于毒性较大,从而限制了它的应用。1974年Dixon发现将丝氨酸、组氨酸接枝到聚乙撑亚胺上,其毒性明显降低,而活性无明显下降。基于聚乙撑亚胺这种性质和联合化疗的思想,我们设想将5-氟尿嘧啶利用氨基酸作为一个桥接枝到聚乙撑亚胺上,得到的接枝物可能具有较高的抗癌活性和较低的毒性。通过5-氟尿嘧啶-1-乙酸对硝基苯酯,5-氟尿嘧啶-1-亚甲基碳酰甘氨酸对硝基苯酚酯,5-氟尿嘧啶-1-亚甲基碳酰苯丙氨酸对硝基苯酚酯分别与聚乙撑亚胺在二甲亚砜中反应,得到三个聚乙撑亚胺的接枝物,通过红外、紫外、元素分析确定了接枝物的结构及组成。
Polyethyleneimine in vivo and in vitro showed some anti-cancer activity, but due to greater toxicity, which limits its application. In 1974, Dixon found that when serine and histidine were grafted onto polyethylenimine, its toxicity was significantly reduced, but its activity was not significantly reduced. Based on the nature of polyethylenimine and the idea of combined chemotherapy, we envisaged that 5-Fluorouracil would utilize amino acids as a bridge to polyethyleneimine and the resulting grafts may have higher anticancer activity and Lower toxicity. P-nitrophenyl 5-fluorouracil-1-acetate, p-nitrophenol 5-fluorouracil-1-methylenecarbodiimide, 5-fluorouracil- Phenol esters were respectively reacted with polyethylenimine in dimethylsulfoxide to obtain three polyethyleneimine grafts. The structure and composition of the grafts were confirmed by infrared, ultraviolet and elemental analysis.