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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