کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364540 | 981539 | 2006 | 7 صفحه PDF | دانلود رایگان |
We report the synthesis of thirty-six Sansalvamide A derivatives, and their biological activity against colon cancer HT-29 cell line, a microsatellite stable (MSS) colon cancer cell-line. The thirty-six compounds can be divided into three subsets, where the first subset of compounds contains l-amino acids, the second subset contains d-amino acids, and the third subset contains both d- and l-amino acids. Five compounds exhibited excellent inhibitory activity (>75% inhibition). The structure–activity relationship (SAR) of the compounds established that a single d-amino acid in position 2 or 3 gave up to a 10-fold improved cytotoxicity over Sansalvamide A peptide. This work highlights the importance of residues 2 and 3 and the role of d-amino acids in the extraordinary SAR for this compound class.
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Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 16, 15 August 2006, Pages 5625–5631