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Bioorg Med Chem Lett. 2004 Mar 22;14(6):1513-7.

Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression.

Author information

1
AtheroGenics, Inc., 8995 Westside Parkway, Alpharetta, GA 30004, USA. cmeng@atherogenics.com

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.

PMID:
15006393
DOI:
10.1016/j.bmcl.2004.01.021
[Indexed for MEDLINE]

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