Preparation and application of biotin-cytarabine prodrug

The invention provides a preparation method and application of a biotin-cytarabine prodrug, and relates to the field of pharmaceutical chemicals. According to the biotin-cytarabine prodrug, a linker is introduced to couple biotin and cytarabine, and a series of biotin-cytarabine prodrugs are prepare...

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Hauptverfasser: JIANG DAOBIN, QIU NENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a preparation method and application of a biotin-cytarabine prodrug, and relates to the field of pharmaceutical chemicals. According to the biotin-cytarabine prodrug, a linker is introduced to couple biotin and cytarabine, and a series of biotin-cytarabine prodrugs are prepared. The reaction conditions are mild, and a series of prepared biotin-cytarabine prodrugs have remarkable beneficial effects. The series of prodrugs are combined with biotin receptors on the surfaces of tumor cells through biotin targeting to enter the tumor cells, and after entering the cells, the prodrugs break through disulfide bonds or amido bonds to release cytarabine to play an anti-tumor role. The biotin-cytarabine prodrug can improve the cytarabine intake of tumor cells, and compared with a cytarabine raw drug, the biotin-cytarabine prodrug has a better killing effect on tumor cells and shows a stronger anti-tumor curative effect. Therefore, the series of biotin-cytarabine prodrugs have good application pros