海洋抗肿瘤候选药物普那布林(Plinabulin)及其类似物的研究进展

The progress of the development of marine antitumor drug Plinabulin and its analogues

微管蛋白是细胞骨架的重要组成部分,在维持形态、信号传导及有丝分裂等过程中起着重要的作用。普那布林(Plinabulin)是在从海洋焦曲霉菌中分离得到的天然产物Phenylahistin结构基础上,经构效关系研究,合成出的二酮哌嗪类微管蛋白抑制剂。普那布林作为抗肿瘤候选药物,目前已进入临床三期研究。近年来,为了获得高效、低毒和生物利用度更高的普那布林衍生物,本领域研究人员进行了大量的优化研究,获得了一些具有更好活性的衍生物。本文就普那布林及其类似物优化的研究进展进行综述。

Tubulin is one of the key components of cytoskeleton and plays an important role in the maintenance of cell shape and the process of signal transduction and mitosis.Plinabulin is a synthesized diketopiperazine derivatives,based on the structure-activity relationship（SAR）study of Phenylahistin which was isolated from Aspergillus.As an antitumor drug candidate,Plinabulin has been pushed into Phase III clinical study.In order to obtain high efficiency,low toxicity and higher bioavailability derivatives of Plinabulin,a number of derivatives have been designed and synthesized in recent years.In this review,the progress of the development of Plinabulin and its analogues was reported.