N-Benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists
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.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.729-733 |
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| container_end_page | 733 |
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| container_issue | 8 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 10 |
| creator | LI CHEN TILLEY, J. W WOLITZKY, B ROWAN, K GUTHRIE, R. W MENNONA, F HUANG, T.-N KAPLAN, G TRILLES, R MIKLOWSKI, D HUBY, N SCHWINGE, V |
| description | 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. |
| doi_str_mv | 10.1016/S0960-894X(00)00089-5 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2000-04, Vol.10 (8), p.729-733 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Enzyme-Linked Immunosorbent Assay Humans Integrin alpha4beta1 Integrins - antagonists & inhibitors Medical sciences Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - chemistry Phenylalanine - pharmacology Receptors, Lymphocyte Homing - antagonists & inhibitors Recombinant Proteins - antagonists & inhibitors Structure-Activity Relationship Vascular Cell Adhesion Molecule-1 - drug effects |
| title | N-Benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists |
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