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鬼臼毒素是一种植物来源的抗肿瘤天然产物,由于其水溶性较差、毒副作用较强且易产生多药耐药性等缺点,使其临床使用受到较大的限制。为了降低毒性、提高活性,国内外研究人员对其结构进行了大量的改造和修饰工作,得到了大量活性优良的鬼臼毒素衍生物,其中以C-4位修饰的产物居多。主要对近3年来鬼臼毒素C-4位结构修饰物的研究进展进行了综述。
Podophyllotoxin is a plant-derived anti-tumor natural product, due to its poor water solubility, strong side effects and easy to produce multi-drug resistance and other shortcomings, its clinical use is subject to greater restrictions. In order to reduce the toxicity and improve the activity, researchers at home and abroad have carried out a great deal of reformation and modification of their structures, and obtained a large number of podophyllotoxin derivatives with excellent activity. Among them, the products modified by C-4 are the most abundant. The research progress of C-4 structure modification of podophyllotoxin in recent 3 years is reviewed.