Discodermolide analogues as the chemical component of combination bacteriolytic therapy

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3623-6. doi: 10.1016/j.bmcl.2005.05.068.

Amos B Smith 3rd ¹, B Scott Freeze, Matthew J LaMarche, Jason Sager, Kenneth W Kinzler, Bert Vogelstein

Affiliations

Affiliation

1 Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, USA.

PMID: 15979874 DOI: 10.1016/j.bmcl.2005.05.068

Abstract

The marine natural product (+)-discodermolide (1) and several simplified analogues of this microtubule-stabilizing agent have proven to be potent in vitro cell growth inhibitory agents in several human Cancer cell lines. Here, we demonstrate the in vivo efficacy of discodermolide and several simplified congeners, both as stand-alone anti-tumor agents and, in the case of (+)-2,3-anhydrodiscodermolide (3), as a chemical component of the combination bacteriolytic therapy. A single intravenous injection of (+)-3 plus genetically modified Clostridium novyi-NT spores caused rapid and complete regressions of tumors in mice bearing HCT116 colorectal Cancer xenografts.

Name
Email *

	Sorry, but the email address you supplied was invalid.