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Bioorganic and Medicinal Chemistry Letters
Volumn 14, Issue 3, 2004, Pages 657-661
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3
Author keywords

Angiogenesis; Cancer; Integrins; Solid phase; v 3
Indexed keywords

PROPIONIC ACID DERIVATIVE; VITRONECTIN RECEPTOR;
EID: 1642493647     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.11.045     Document Type: Article
Times cited : (9)
References (25)
  • 1
  • 21
    • 85030912485 scopus 로고    scopus 로고
    • Chemical stability was measured on the final compounds, in the Tris buffer, pH 7.4, used for the biochemical assays
    • Chemical stability was measured on the final compounds, in the Tris buffer, pH 7.4, used for the biochemical assays.
  • 23
    • 15844420283 scopus 로고    scopus 로고
    • Briefly, the integrin was coated onto a 96-well plate (50 mg/well) and 5 nM biotinylated vitronectin was allowed to bind for 30 min at 37 °C, with or without increasing concentrations of the competing molecules. The plate was then rinsed and incubated 45 min with streptavidin conjugated to peroxidase. The amount of vitronectin bound was monitored after addition of Turbo-TMB as peroxidase substrate, and the yellow color produced was read by a Packard ELISA reader, at 450 nm wavelength. Data were analyzed using the computerized program 'GraphPad Prism'
    • Brooks P.C., Stromblad S., Sanders L.C., von Schalscha T.L., Aimes R.T., Stetler-Stevenson W.G., Quigley J.P., Cheresh D.A. Cell. 85:1996;683. Briefly, the integrin was coated onto a 96-well plate (50 mg/well) and 5 nM biotinylated vitronectin was allowed to bind for 30 min at 37 °C, with or without increasing concentrations of the competing molecules. The plate was then rinsed and incubated 45 min with streptavidin conjugated to peroxidase. The amount of vitronectin bound was monitored after addition of Turbo-TMB as peroxidase substrate, and the yellow color produced was read by a Packard ELISA reader, at 450 nm wavelength. Data were analyzed using the computerized program 'GraphPad Prism'.
    • (1996) Cell , vol.85 , pp. 683
    • Brooks, P.C.1    Stromblad, S.2    Sanders, L.C.3    Von Schalscha, T.L.4    Aimes, R.T.5    Stetler-Stevenson, W.G.6    Quigley, J.P.7    Cheresh, D.A.8
  • 24
    • 85030896533 scopus 로고    scopus 로고
    • 2). Then, 10 μL of adhesion medium containing inhibitors at suitable concentrations were added to test wells. 90 μL/well of cell suspension was plated and incubated for 1 h at 37 °C. Following adhesion, plates were gently washed and cells fixed with 50 μL TCA 50% (trichloroacetic acid). Evaluation of cell adhesion was performed by staining with sulforhodamine B
    • 2). Then, 10 μL of adhesion medium containing inhibitors at suitable concentrations were added to test wells. 90 μL/well of cell suspension was plated and incubated for 1 h at 37 °C. Following adhesion, plates were gently washed and cells fixed with 50 μL TCA 50% (trichloroacetic acid). Evaluation of cell adhesion was performed by staining with sulforhodamine B.
  • 25
    • 85030891212 scopus 로고    scopus 로고
    • CEMD9 is a recombinant sub-line, derived from an acute lymphoblastic leukemia (ATCC CCL-119), stably expressing αvβ3 integrin obtained by co-transfecting cDNAs encoding human αv and β3 subunits. Cells were dispensed in 96 wells and treatment was performed 2 h later. Evaluation of growing inhibition was done 72 h later
    • CEMD9 is a recombinant sub-line, derived from an acute lymphoblastic leukemia (ATCC CCL-119), stably expressing αvβ3 integrin obtained by co-transfecting cDNAs encoding human αv and β3 subunits. Cells were dispensed in 96 wells and treatment was performed 2 h later. Evaluation of growing inhibition was done 72 h later.

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