abstract |
The cytarabine prodrug derivatives of general formula (I), their synthetic routes, preparation and preparative method thereof, and use for resisting cancer or tumor. The derivatives are prepared by chemical modification on N4, O5 positions of cytarabine, which can avoid losing efficacy and inducing toxicity caused by N4-amino group metabolism, and make O5-hydroxy group be easily phosphorylated and activated. The derivatives can increase bioavailability, solubility and liposolubility, and reduce multidrug resistance. |