Derivatives of tetrahydroisoquinoline: Synthesis and initial evaluation of novel non-peptide antagonists of the αIIbβ3-integrin
| Autor: | Tatyana A. Kabanova, V. M. Kabanov, A. A. Krysko, Olga L. Krysko, Sergei A. Andronati |
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| Rok vydání: | 2010 |
| Předmět: |
Platelet Aggregation
Stereochemistry Clinical Biochemistry Pharmaceutical Science Platelet Glycoprotein GPIIb-IIIa Complex Biochemistry Chemical synthesis chemistry.chemical_compound Tetrahydroisoquinolines Drug Discovery Humans Potency Platelet Molecular Biology Bicyclic molecule Chemistry Cell adhesion molecule Tetrahydroisoquinoline Organic Chemistry Antagonist Fibrinogen In vitro Molecular Medicine Oligopeptides Fluorescein-5-isothiocyanate Platelet Aggregation Inhibitors Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:4444-4446 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.06.051 |
| Popis: | The novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-4-oxobutyric or 5-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-5-oxopentanoic acids as a surrogate of Arg-Gly motif. The synthesized compounds have demonstrated a high potency to inhibit platelet aggregation in vitro and to block FITC-Fg binding to α IIb β 3 on washed human platelets. |
| Databáze: | OpenAIRE |
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