Davis Melinda R, Styers Thomas J, Rodriguez Rodrigo A, Pan Po-Shen, Vasko Robert C, McAlpine Shelli R
Department 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.
Org Lett. 2008 Jan 17;10(2):177-80. doi: 10.1021/ol702403r. Epub 2007 Dec 21.
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.
本文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。这些衍生物是通过简洁的汇聚合成法制备的。这些类似物与目前的癌症药物没有结构同源性，其细胞毒性水平与现有癌症治疗药物相当，并且对耐药胰腺癌细胞系比对非癌细胞系表现出选择性。这些分子是寻找新型抗癌药物的优秀化疗先导物。
