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

Authors :
Meng CQ
Zheng XS
Ni L
Ye Z
Simpson JE
Worsencroft KJ
Hotema MR
Weingarten MD
Skudlarek JW
Gilmore JM
Hoong LK
Hill RR
Marino EM
Suen KL
Kunsch C
Wasserman MA
Sikorski JA
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Mar 22; Vol. 14 (6), pp. 1513-7.
Publication Year :
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.

Details

Language :
English
ISSN :
0960-894X
Volume :
14
Issue :
6
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
15006393
Full Text :
https://doi.org/10.1016/j.bmcl.2004.01.021