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- W2024951966 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." @default.
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- W2024951966 date "2011-10-01" @default.
- W2024951966 modified "2023-10-16" @default.
- W2024951966 title "Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells" @default.
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- W2024951966 doi "https://doi.org/10.1016/j.bmcl.2011.07.079" @default.
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