Synthesis and cytotoxicity of a new class of potent decapeptide macrocycles
Synthesis and cytotoxicity of a new class of potent decapeptide macrocycles
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DOI：
10.1021/ol702403r
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发表时间：
2008-01-17
期刊：
影响因子：
5.2
通讯作者：
McAlpine, Shelli R.
中科院分区：
文献类型：
--
作者：
Davis, Melinda R.;Styers, Thomas J.;McAlpine, Shelli R.
描述了五种十肽的合成，它们是天然产物五肽Sansalvamide A的C-2-对称衍生物。衍生物是使用简洁的聚合合成法制备的。这些类似物与当前的癌症药物没有结构同源性，其细胞毒性水平与现有的治疗癌症的药物相当，并且表现出对耐药胰腺癌细胞系相对于非癌细胞系的选择性。这些分子是寻找新抗癌药物的优秀化疗先导药物。
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.