Podophyllotoxin derivatives targeting tubulin: An update (2017-2022)

Numerous tubulin-targeted podophyllotoxin congeners have been designed and synthesized to overcome the poor water solubility of podophyllotoxin and improve its pharmaceutical characteristics. Understanding the interaction of tubulin with its downstream signal transduction pathways is important for insights into the role of tubulin in the anticancer action of podophyllotoxin-based conjugates. In this review, we provide a detailed account of recent advances in tubulin targetingpodophyllotoxin derivatives with a focus on their antitumor action and potential molecular signaling pathways directly involved in tubulin depolymerization. Such information will be of benefit to researchers designing and developing anticancer drugs derived from podophyllotoxin. Moreover, we also discuss the associated challenges and future opportunities in this field.

Automated summary

Numerous tubulin-targeted podophyllotoxin congeners have been developed to enhance the pharmaceutical properties of podophyllotoxin. Understanding the interaction between tubulin and its downstream signaling pathways is crucial for comprehending the anticancer mechanism of podophyllotoxin-based conjugates. This review provides a comprehensive overview of recent advancements in tubulin-targeting podophyllotoxin derivatives, particularly their antitumor activities and the potential molecular signaling pathways involved in tubulin depolymerization. This information is valuable for researchers involved in the design and development of anticancer drugs derived from podophyllotoxin. Additionally, challenges and future perspectives in this field are also discussed.