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Diamine containing VLA-4 antagonists
P C Astles1, N V Harris, A D Morley
1Aventis Pharma Ltd, Dagenham Research Centre, Dagenham, RM10 7XS, Essex, UK.
Bioorganic & Medicinal Chemistry
|August 16, 2001
Abstract:
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 <10 nmol for inhibiting the VLA-4 mediated binding of fibronectin to RAMOS cells, providing an ideal starting point for a lead optimisation Programme.