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Nitrobenzene compounds inhibit expression of VCAM-1.

Meng, C Q; Zheng, X S; Holt, L A; Hoong, L K; Somers, P K; Hill, R R; Saxena, U.

Bioorg Med Chem Lett ; 11(14): 1823-7, 2001 Jul 23.

Article in English | MEDLINE | ID: mdl-11459640

ABSTRACT

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.

Subject(s)

Intercellular Adhesion Molecule-1/drug effects , Nitrobenzenes/chemical synthesis , Nitrobenzenes/pharmacology , Vascular Cell Adhesion Molecule-1/drug effects , Autoimmune Diseases/drug therapy , Cells, Cultured/cytology , Electron Transport , Endothelium/cytology , Humans , Hypersensitivity/drug therapy , Inflammation/drug therapy , Inhibitory Concentration 50 , Integrin alpha4beta1 , Integrins/metabolism , Receptors, Lymphocyte Homing/metabolism , Structure-Activity Relationship , Vascular Cell Adhesion Molecule-1/biosynthesis , Vascular Cell Adhesion Molecule-1/genetics

ABSTRACT

Subject(s)

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