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Review Article

小分子吉西他滨前药用于癌症治疗

卷 27, 期 33, 2020

页: [5562 - 5582] 页: 21

弟呕挨: 10.2174/0929867326666190816230650

价格: $65

摘要

吉西他滨作为嘧啶核苷类似物的抗癌药对广泛的实体瘤具有很高的疗效。 吉西他滨在肿瘤细胞内被脱氧胞苷激酶依次磷酸化为单磷酸，二磷酸和三磷酸核苷酸，最后一个为活性形式，从而被激活。 但是其不稳定性，耐药性和毒性严重限制了其在临床中的应用。 在药物化学领域，已证明前药是提高药物稳定性和减少不良副作用的非常有效的手段，包括核苷抗癌药如吉西他滨。 吉西他滨前药的设计和合成已完成许多工作，本综述总结了其中的大多数。

关键词: 吉西他滨，前药，酰胺，酯，衍生物，抗癌药。

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