Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 24, Pages 7537-7539Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.075
Keywords
Matrine; Pro-inflammatory cytokine; NF kappa B; Derivatives; SAR
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Funding
- National Nature Science Foundation of China [30783087]
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Matrine, a sophora alkaloid, exhibited good anti-inflammation effects in our previous report. In the present study, a series of matrine derivatives were synthesized via classical Michael addition. Biological studies showed that the synthetic derivatives had good inhibitory effect towards TNF-alpha production and NF kappa B transcriptional activity. The introduction of various amino groups to the keto beta position could improve the biochemical profile, resulting in the identification of more potent derivates, such as 1f, with higher inhibitory activity than both matrine and sophoramine. (C) 2010 Published by Elsevier Ltd.
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