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 gro...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (14), p.1823-1827
Main Authors: MENG, Charles Q, ZHENG, X. Sharon, HOLT, Lisa A, HOONG, Lee K, SOMERS, Patricia K, HILL, Russell R, SAXENA, Uday
Format: Article
Language:English
Subjects:
Autoimmune Diseases - drug therapy
Biological and medical sciences
Cells, Cultured - cytology
Electron Transport
Endothelium - cytology
Humans
Hypersensitivity - drug therapy
Immunomodulators
Inflammation - drug therapy
Inhibitory Concentration 50
Integrin alpha4beta1
Integrins - metabolism
Intercellular Adhesion Molecule-1 - drug effects
Medical sciences
Nitrobenzenes - chemical synthesis
Nitrobenzenes - pharmacology
Pharmacology. Drug treatments
Receptors, Lymphocyte Homing - metabolism
Structure-Activity Relationship
Vascular Cell Adhesion Molecule-1 - biosynthesis
Vascular Cell Adhesion Molecule-1 - drug effects
Vascular Cell Adhesion Molecule-1 - genetics
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00306-7