Abstract
A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA assay and low-microM activity in a cell based assay.
MeSH terms
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Cell Line
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Enzyme-Linked Immunosorbent Assay
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Humans
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Integrin alpha4beta1
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Integrins / antagonists & inhibitors*
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Phenylalanine / analogs & derivatives*
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Phenylalanine / chemistry
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Phenylalanine / pharmacology
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Receptors, Lymphocyte Homing / antagonists & inhibitors*
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
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Vascular Cell Adhesion Molecule-1 / drug effects*
Substances
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Integrin alpha4beta1
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Integrins
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Receptors, Lymphocyte Homing
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Recombinant Proteins
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Vascular Cell Adhesion Molecule-1
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Phenylalanine