title: N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
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.
authors.affiliation: Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA.
authors.forename: L
authors.initials: L
authors.lastname: Chen
authors.forename: J W
authors.initials: JW
authors.lastname: Tilley
authors.forename: R W
authors.initials: RW
authors.lastname: Guthrie
authors.forename: F
authors.initials: F
authors.lastname: Mennona
authors.forename: T N
authors.initials: TN
authors.lastname: Huang
authors.forename: G
authors.initials: G
authors.lastname: Kaplan
authors.forename: R
authors.initials: R
authors.lastname: Trilles
authors.forename: D
authors.initials: D
authors.lastname: Miklowski
authors.forename: N
authors.initials: N
authors.lastname: Huby
authors.forename: V
authors.initials: V
authors.lastname: Schwinge
authors.forename: B
authors.initials: B
authors.lastname: Wolitzky
authors.forename: K
authors.initials: K
authors.lastname: Rowan
mesh_terms: D002460:Cell Line; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D019010:Vascular Cell Adhesion Molecule-1 / Q000187:drug effects*
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; D016201:Receptors, Lymphocyte Homing; D011994:Recombinant Proteins; D019010:Vascular Cell Adhesion Molecule-1; D010649:Phenylalanine