Abstract

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.

Keywords: Podophyllotoxin, Epipodophyllotoxin, Anticancer, Multidrug resistance, Mechanism of action, Structure-activity relationship.

Graphical Abstract