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Org Lett. 2008 Jan 17;10(2):177-80. Epub 2007 Dec 21.

Synthesis and cytotoxicity of a new class of potent decapeptide macrocycles.

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  • 1Department of Chemistry, Molecular Biology Institute, and Center for Applied and Experimental Genomics, 5500 Campanile Road, 208 CSL, San Diego State University, San Diego, California 92182-1030, USA.


Described are the syntheses of five decapeptides that are C-2-symmetrical derivatives of the natural product pentapeptide sansalvamide A. Derivatives were made using a succinct convergent synthesis. These analogues share no structural homology to current cancer drugs, are cytotoxic at levels on par with existing drugs treating cancers, and demonstrate selectivity for drug-resistant pancreatic cancer cell lines over noncancerous cell lines. These molecules are excellent chemotherapeutic leads in the search for new anticancer agents.

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