College of Medicine, Xuchang University, Xuchang, China.
Institutes of Nursing and Health, Henan Medical School, Henan University, Kaifeng, China.
Curr Top Med Chem. 2021;21(19):1712-1724. doi: 10.2174/1568026621666210113163327.
Podophyllotoxins, including epipodophyllotoxin derivatives, can act on a diverse array of drug targets in cancer cells and thus possess potent activity against various forms of cancer cell lines, including drug-resistant forms. Moreover, several podophyllotoxin derivatives represented by etoposide and teniposide, have already been approved for cancer therapy, demonstrating podophyllotoxin moiety as a useful pharmacophore for the discovery of novel anticancer agents. This review reports the recent advances in the exploitation of podophyllotoxin derivatives to fight against multidrug-resistant cancer cells. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted.
鬼臼毒素及其衍生物可作用于癌细胞中的多种药物靶点,因此对多种形式的癌细胞系具有很强的活性,包括耐药形式。此外,依托泊苷和替尼泊苷等几种鬼臼毒素衍生物已被批准用于癌症治疗,这表明鬼臼毒素部分是发现新型抗癌药物的有用药效团。本文综述了鬼臼毒素衍生物在对抗多药耐药癌细胞方面的最新研究进展。还强调了作用机制和构效关系(SAR)研究。