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Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers.

ABSTRACT: A series of novel ether-linked dimers of demethylepipodophyllotoxin are topoisomerase II poisons that exhibit higher levels of double-stranded versus single-stranded DNA cleavage than their corresponding monomers. The dimers also have higher levels of tumor cell cytotoxicity than the monomers, lending support to the two-drug model for interaction of demethylepipodophyllotoxins with human topoisomerase II?.

SUBMITTER: Dunlap N

PROVIDER: S-EPMC4425371 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers.

Dunlap Norma N Salyard Tracy L J TLJ Pathiranage Anuradha Liyana AL Stubblefield Jeannie J Pitts Steven L SL Ashley Rachel E RE Osheroff Neil N

Bioorganic & medicinal chemistry letters 20141101 24

A series of novel ether-linked dimers of demethylepipodophyllotoxin are topoisomerase II poisons that exhibit higher levels of double-stranded versus single-stranded DNA cleavage than their corresponding monomers. The dimers also have higher levels of tumor cell cytotoxicity than the monomers, lending support to the two-drug model for interaction of demethylepipodophyllotoxins with human topoisomerase IIα. ...[more]

PMID: 25466187

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