Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1497-9. doi: 10.1016/s0960-894x(00)00300-0.

Abstract

Several phenylalanine based inhibitors were synthesized as antagonists of the leukocyte cell adhesion process that is mediated through the interactions of the mucosal addressin cell adhesion molecule (MAdCAM) and the integrin alpha4beta7. Analogues 20, 21, 22 and 24 displayed inhibition of adhesion in a cell based assay in the low micromolar range.

MeSH terms

  • Cell Adhesion / drug effects*
  • Cell Adhesion Molecules
  • Humans
  • Immunoglobulins / physiology*
  • Integrins / antagonists & inhibitors
  • Integrins / physiology*
  • Lymphoma, B-Cell
  • Molecular Structure
  • Mucoproteins / physiology*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemical synthesis
  • Phenylalanine / pharmacology*
  • Receptors, Lymphocyte Homing / antagonists & inhibitors
  • Receptors, Lymphocyte Homing / physiology
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Cell Adhesion Molecules
  • Immunoglobulins
  • Integrins
  • MADCAM1 protein, human
  • Mucoproteins
  • Receptors, Lymphocyte Homing
  • integrin alpha4beta7
  • Phenylalanine