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Diamine containing VLA-4 antagonists

Astles, P C ; Harris, N V ; Morley, A D

Bioorganic & medicinal chemistry, August 2001, Vol.9(8), pp.2195-202 [Peer Reviewed Journal]

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  • Title:
    Diamine containing VLA-4 antagonists
  • Author: Astles, P C ; Harris, N V ; Morley, A D
  • Description: 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.
  • Is Part Of: Bioorganic & medicinal chemistry, August 2001, Vol.9(8), pp.2195-202
  • Identifier: ISSN: 0968-0896 ; PMID: 11504657 Version:1
  • Subjects: Diamines -- Chemical Synthesis ; Integrins -- Antagonists & Inhibitors ; Receptors, Lymphocyte Homing -- Antagonists & Inhibitors
  • Language: English

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