Diamine containing VLA-4 antagonists.

P C Astles; N V Harris; A D Morley

doi:10.1016/s0968-0896(01)00132-8

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PubMed · 11504657

Diamine containing VLA-4 antagonists.

P C Astles·N V Harris·A D Morley

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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.

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Cell Adhesion Diamines Drug Design Humans Integrin alpha4beta1 Integrins Receptors, Lymphocyte Homing Structure-Activity Relationship Tumor Cells, Cultured Journal Article

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P C Astles, N V Harris, A D Morley. 2001. Diamine containing VLA-4 antagonists.. https://doi.org/10.1016/s0968-0896(01)00132-8

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