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乙双哌嗪二酮(Ⅰ,乙亚胺)是近年来发现的一类新型抗癌药。其毒性较小,在动物实验中显示明显的抗瘤作用,并能阻止肿瘤四周的血管形成,防止癌细胞的转移,但其水溶性太小,口服吸收不佳,临床疗效不很理想。为了寻找临床有用的抗癌药,乃将Ⅰ的结构进行改变。鉴于哌嗪二酮类化合物中酰亚胺氮上的氢原子若以烷基取代,可以增加化合物的水溶性;又鉴
B piperazine dione (Ⅰ, ethylene imine) is a new type of anticancer drug discovered in recent years. Its toxicity is small, showing obvious anti-tumor effect in animal experiments, and can prevent the formation of blood vessels around the tumor and prevent the metastasis of cancer cells. However, its water solubility is too small and oral absorption is poor, and the clinical curative effect is not very satisfactory. In order to find a clinically useful anticancer drug, the structure of I was changed. Given the piperazine dione compound imide nitrogen hydrogen atoms on the alkyl substitution, can increase the water solubility of compounds; also Kam