Journal
TETRAHEDRON LETTERS
Volume 55, Issue 51, Pages 6979-6982Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2014.10.089
Keywords
Sanguinamide B; Macrocycle; Heterocycle; Natural product; Conformation; Peptide
Categories
Funding
- Australian National Health and Medical Research Council (NHMRC) [APP1043561]
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available