Synthesis and Cytotoxicity of a New Class of Potent Decapeptide Macrocycles

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• 作者：Melinda R. Davis ; Thomas J. Styers ; Rodrigo A. Rodriguez ; Po-Shen Pan ; Robert C. Vasko ; Shelli R. McAlpine
• 刊名：Organic Letters
• 出版年：2008
• 出版时间：January 17, 2008
• 年：2008
• 卷：10
• 期：2
• 页码：177 - 180
• 全文大小：155K
• 年卷期：v.10,no.2(January 17, 2008)
• ISSN：1523-7052

文摘

ABLE>als/orlef7/10/i02/figures/ol702403rn00001.gif" ALIGN="left" HSPACE=5>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, arecytotoxic at levels on par with existing drugs treating cancers, and demonstrate selectivity for drug-resistant pancreatic cancer cell lines overnoncancerous cell lines. These molecules are excellent chemotherapeutic leads in the search for new anticancer agents.