吉西他滨衍生物抗肿瘤活性的研究进展

Research Advances in the Anti-tumor Activities of Gemcitabine Derivatives

吉西他滨作为恶性肿瘤临床治疗一线药物,目前存在不能口服、易被脱氨酶代谢、生物利用度低、易产生耐药性等缺陷。近年来,为了改善吉西他滨的上述缺陷,研究者们利用前药设计策略,对其进行了大量的结构修饰。详细介绍了吉西他滨衍生物的最新研究进展,以期为获得改善临床缺陷的新型吉西他滨衍生物提供参考。

As the first-line therapy of malignant tumor, gemcitabine is compromised by inability to be taken orally, rapid metabolism by deaminase, low bioavailability and easy development of drug resistance. To circumvent these shortcomings, researchers have devoted continuous efforts to structure modification of gemcitabine using prodrug strategy. This review summarizes the latest advances in gemcitabine derivatives and expects to provide reference for the development of new gemcitabine derivatives to overcome clinical shortcomings.