Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells. (Articolo in rivista)

Type
Label
  • Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells. (Articolo in rivista) (literal)
Anno
  • 2011-01-01T00:00:00+01:00 (literal)
Alternative label
  • Radi M, Brullo C, Crespan E, Tintori C, Musumeci F, Biava M, Schenone S, Dreassi E, Zamperini C, Maga G, Pagano D, Angelucci A, Bologna M, Botta M. (2011)
    Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.
    in Bioorganic & medicinal chemistry letters (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Radi M, Brullo C, Crespan E, Tintori C, Musumeci F, Biava M, Schenone S, Dreassi E, Zamperini C, Maga G, Pagano D, Angelucci A, Bologna M, Botta M. (literal)
Pagina inizio
  • 5928 (literal)
Pagina fine
  • 5933 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 12 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • University of Siena, Italy IGM-CNR, Pavia, Italy University of Genova, Italy (literal)
Titolo
  • Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells. (literal)
Abstract
  • Neuroblastoma (NB) represents the most common extracranial paediatric solid tumor for which no specific FDA-approved treatment is currently available. The tyrosine kinase c-Src has been reported to play an important role in the differentiation, cell-adhesion and survival of NB cells. Starting from dual Src/Abl inhibitors previously found active in NB cell lines (1-3), small modification of the original structures almost abolished the Abl activity with a contemporary improvement of affinity and specificity for c-Src. Among the synthesized compounds, the most potent c-Src inhibitor (10a) showed a very interesting antiproliferative activity in SH-SY5Y cells with an IC(50) of 80 nM and a favourable ADME profile. A 3D SAR analysis was also attempted and may guide the design of more potent c-Src inhibitors as potential agents for NB treatment. (literal)
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