Synthesis and Cytotoxicity of a New Class of Potent Decapeptide Macrocycles
Organic Letters2007Vol. 10(2), pp. 177–180
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Melinda R. Davis, Thomas J. Styers, Rodrigo A. Rodriguez, Po‐Shen Pan, Robert C. Vasko, Shelli R. McAlpine
Abstract
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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