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On-Chip Endothelial Inflammatory Phenotyping
Published on: July 22, 2012
Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression
Charles Q Meng1, X Sharon Zheng, Liming Ni
1AtheroGenics, Inc., 8995 Westside Parkway, Alpharetta, GA 30004, USA. cmeng@atherogenics.com
Bioorganic & Medicinal Chemistry Letters
|March 10, 2004
Abstract:
Novel chalcone derivatives have been discovered as potent inhibitors of TNF-alpha-induced VCAM-1 expression. Thienyl or benzothienyl substitution at the meta-position of ring B helps boost potency while large substitution at the para-position on ring B is detrimental. Various substitutions are tolerated on ring A. A lipophilicity-potency relationship has been observed in several sub-series of compounds.
