Podophyllotoxins including epipodophyllotoxin derivatives can act on a diverse array
of drug targets in cancer cells, and thus possess potential activity against various forms of cancer
cell lines including drug-resistant forms. Moreover, several podophyllotoxin derivatives which are
represented by etoposide and teniposide have already been approved for the cancer therapy,
demonstrating podophyllotoxin moiety is a useful pharmacophore for the discovery of novel
anticancer agents. This review reports the recent advances in 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.
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