Podophyllotoxins and epipodophyllotoxins, possess excellent activity against both drug-sensitive and drug-resistant even multidrug-resistant cancer cells via inhibition of tubulin polymerization. Several podophyllotoxin/epipodophyllotoxin derivatives such as etoposide and teniposide have already been applied for cancer therapy, revealing their potential as putative anticancer drugs. Hybridization of podophyllotoxin/epipodophyllotoxin moiety with other anticancer pharmacophores is a promising strategy to develop novel drug candidates so as to overcome drug resistance and improve the specificity, and numerous of podophyllotoxin/epipodophyllotoxin hybrids exhibit excellent in vitro antiproliferative and in vivo anticancer potency. This review emphasizes the recent development of podophyllotoxin/epipodophyllotoxin hybrids with potential application for cancer therapy covering articles published between 2010 and 2020. The mechanisms of action, the critical aspects of design as well as structure-activity relationships were also summarized.

鬼臼毒素和鬼臼毒素通过抑制微管蛋白的聚合，对药物敏感性和耐药性甚至对多药耐药的癌细胞均具有优异的活性。几种鬼臼毒素/表鬼臼毒素衍生物（如依托泊苷和替尼泊苷）已被用于癌症治疗，显示出它们作为潜在的抗癌药物的潜力。鬼臼毒素/表鬼臼毒素与其他抗癌药效团的杂交是开发新的候选药物从而克服耐药性并提高特异性的有前途的策略，并且许多鬼臼毒素/鬼臼毒素的杂种均表现出优异的体外抗增殖和体内活性抗癌效力。这篇综述强调了鬼臼毒素/表鬼臼毒素杂种的最新发展及其在癌症治疗中的潜在应用，涵盖了2010年至2020年之间发表的文章。还总结了作用机理，设计的关键方面以及结构与活性之间的关系。