Nitrobenzene compounds inhibit expression of VCAM-1.
A series of nitrobenzene compounds has been discovered as potent inhibitors of VCAM-1 expression and, therefore, potential drug candidates for autoimmune and allergic inflammatory diseases. Structure-activity relationship (SAR) studies showed that a nitro group and two other electron-withdrawing groups are essential for these compounds to be potent inhibitors of VCAM-1 expression.
Meng
C Q
CQ
AtheroGenics, Inc., 8995 Westdise Parkway, 30004, Alpharetta, GA, USA. cmeng@atherogenics.com
Zheng
X S
XS
Holt
L A
LA
Hoong
L K
LK
Somers
P K
PK
Hill
R R
RR
Saxena
U
U
D001327:Autoimmune Diseases / Q000188:drug therapy; D002478:Cells, Cultured / Q000166:cytology; D004579:Electron Transport; D004727:Endothelium / Q000166:cytology; D006801:Humans; D006967:Hypersensitivity / Q000188:drug therapy; D007249:Inflammation / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D039041:Integrin alpha4beta1; D016023:Integrins / Q000378:metabolism; D018799:Intercellular Adhesion Molecule-1 / Q000187:drug effects*; D009578:Nitrobenzenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D016201:Receptors, Lymphocyte Homing / Q000378:metabolism; D013329:Structure-Activity Relationship; D019010:Vascular Cell Adhesion Molecule-1 / Q000096:biosynthesis / Q000187:drug effects* / Q000235:genetics
D039041:Integrin alpha4beta1; D016023:Integrins; D009578:Nitrobenzenes; D016201:Receptors, Lymphocyte Homing; D019010:Vascular Cell Adhesion Molecule-1; D018799:Intercellular Adhesion Molecule-1