Diamine containing VLA-4 antagonists

Diamine containing VLA-4 antagonists

Design and synthesis of a library as potential VLA-4 antagonists has been accomplished, based around a proposed pharmacophoric model. Compounds possessing submicromolar potency were identified and structure–activity relationships were seen across the library. Further derivatisation produced compound...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2001-08, Vol.9 (8), p.2195-2202
Hauptverfasser: Astles, Peter C., Harris, Neil V., Morley, Andrew D.
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cell Adhesion - drug effects
Diamines - chemical synthesis
Diamines - chemistry
Diamines - pharmacology
Drug Design
Humans
Integrin alpha4beta1
Integrins - antagonists & inhibitors
Integrins - chemistry
Medical sciences
Pharmacology. Drug treatments
Receptors, Lymphocyte Homing - antagonists & inhibitors
Receptors, Lymphocyte Homing - chemistry
Structure-Activity Relationship
Tumor Cells, Cultured
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Zusammenfassung:Design and synthesis of a library as potential VLA-4 antagonists has been accomplished, based around a proposed pharmacophoric model. Compounds possessing submicromolar potency were identified and structure–activity relationships were seen across the library. Further derivatisation produced compounds with IC 50's
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(01)00132-8