Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5627-5629. doi: 10.1016/j.bmcl.2014.10.082.

Norma Dunlap ¹, Tracy L J Salyard ¹, Anuradha Liyana Pathiranage ¹, Jeannie Stubblefield ¹, Steven L Pitts ², Rachel E Ashley ², Neil Osheroff ²

Affiliations

1 Department of Chemistry, Middle Tennessee State University, 1301 Main St., Murfreesboro, TN, USA.
2 Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN, USA.

PMID: 25466187 DOI: 10.1016/j.bmcl.2014.10.082

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 IIα.

Keywords

Cytotoxicity; Demethylepipodophyllotoxin; Topoisomerase.

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