期刊
TETRAHEDRON LETTERS
卷 55, 期 51, 页码 6979-6982出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2014.10.089
关键词
Sanguinamide B; Macrocycle; Heterocycle; Natural product; Conformation; Peptide
资金
- Australian National Health and Medical Research Council (NHMRC) [APP1043561]
We report the synthesis of seven new sanguinamide B (SanB) analogues. Substitution of amino acids along the backbone of SanB and testing in HCT-116 colon cancer cell lines identified new biologically active SanB derivatives. These compounds establish a structure activity relationship and show that a Cbz-lysine moiety is important for biological activity. We also identified the most effective stereochemistry at each position around the molecule. The biological activity of the macrocycle is extremely sensitive to stereochemistry and amino acid placement. (C) 2014 Elsevier Ltd. All rights reserved.
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