Synthesis and cytotoxicity of a new class of potent decapeptide macrocycles

被引：20

作者：

Davis, Melinda R. ^{[1
,2
]}

Styers, Thomas J. ^{[1
,2
]}

Rodriguez, Rodrigo A. ^{[1
,2
]}

Pan, Po-Shen ^{[1
,2
]}

Vasko, Robert C. ^{[1
,2
]}

McAlpine, Shelli R. ^{[1
,2
]}

机构：

[1] San Diego State Univ, Dept Chem, Inst Mol Biol, San Diego, CA 92182 USA

[2] San Diego State Univ, Ctr Appl & Expt Genom, San Diego, CA 92182 USA

来源：

ORGANIC LETTERS | 2008年 / 10卷 / 02期

关键词：

D O I：

10.1021/ol702403r

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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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页码：177 / 180

页数：4

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