维甲酰阿糖胞苷缀合物及其药质体、其制备方法和应用技术

本发明专利技术公开具有两亲性的维甲酰阿糖胞苷缀合物以及由该缀合物构建而得的药质体，本发明专利技术还公开了它们的制备方法以及它们作为抗肿瘤剂的应用。本发明专利技术将全反式维甲酸与阿糖胞苷４’位氨基偶联，获得具有两亲性的维甲酰阿糖胞苷缀合物，该缀合物具备自组装为药质体的特性，既可保护阿糖胞苷４’位氨基失活，又可使该缀合物及所制备的药质体具有肿瘤靶向性。本发明专利技术分别用人白血病细胞ＨＬ－６０和Ｓ↓［１８０］腹水癌小鼠评价了本发明专利技术式Ⅰ化合物及由该化合物所制备药质体的体外和体内抗肿瘤活性，实验结果表明，本发明专利技术式Ⅰ化合物及其药质体具有优秀的抗肿瘤活性。

Conjugate of cytarabine cytosine and its drug body, preparation method and application thereof

The present invention discloses a conjugate of two vitamin cytosine arabinoside and a drug plasmid constructed from the conjugate, and also discloses a method for preparing the same and their use as antitumor agents. The invention of all trans retinoic acid and cytarabine 4 'amino coupling with two amphipathic dimensional formyl cytarabine conjugates, the conjugates have self assembling properties for pharmacosome, which can protect the cytarabine 4' amino inactivation, and can make the conjugates and the pharmacosomes prepared with tumor targeting. The present invention respectively with human leukemia cell line HL 60 and S: 180 ascites carcinoma of the invention of compounds were evaluated by the compound and preparation of pharmacosomes in vitro and in vivo antitumor activity, the experimental results show that the compound of formula I and pharmacosome has excellent anti tumor activity.

【技术实现步骤摘要】

【技术保护点】
维甲酰阿糖胞苷缀合物，其结构式为式Ⅰ所示：　＊＊＊　式Ⅰ。

【技术特征摘要】

【专利技术属性】
技术研发人员：崔国辉，崔纯莹，张云玮，
申请(专利权)人：首都医科大学，
类型：发明
国别省市：11[中国|北京]