Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 19, Pages 5653-5657Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.033
Keywords
Parallel synthesis; Solid phase synthesis; Natural cyclopeptides; Anti-inflammatory activity
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Funding
- NIH [1R03DA025850-01A1, 5P41GM081261-03, 3P41GM079590-03S1]
- JDRF
- MSNRC
- State of Florida
- Tunisian Ministry of Higher Education
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We report the parallel synthesis of two natural cyclopeptides, isolated from the seeds of Annona squamosa, cyclosquamosin D (A1), and Met-cherimolacyclopeptide B (B) and their analogs. All of the compounds were screened for anti-inflammatory activity by evaluating their inhibitory effects on the production of pro-inflammatory cytokines using the lipopolysaccharide stimulated macrophage J774A.1 cell line. Compounds having significant anti-inflammatory activity in suppressing the secretion of IL-6 and TNF-alpha have been identified, some of which exhibit activity superior to that observed with the natural products. (C) 2010 Elsevier Ltd. All rights reserved.
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