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Title: Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells.
Authors: Botta, Maurizio 
Brullo, C.
Crespan, E.
Tintori, Cristina
Musumeci, F.
Biava, M.
Schenone, S.
Dreassi, Elena 
Zamperini, Claudio
Maga, G.
Pagano, D.
Angelucci, A.
Bologna, M.
Botta, Maurizio 
Keywords: Neuroblastoma, c-Src, Bcr-Abl, Kinase, Pyrazolo[3; 4-d]pyrimidines
Issue Date: 2011
Project: None 
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 IC50 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.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2011.07.079
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