Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.

@article{Pl2004DiscoveryOA,
  title={Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.},
  author={Patrick A Pl{\'e} and Tim P. Green and Laurent François Hennequin and Jon O. Curwen and Michael Fennell and Jack E. Allen and Christine Lambert-van der Brempt and Gerard F Costello},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 4},
  pages={871-87}
}
Deregulated activity of the nonreceptor tyrosine kinase c-Src is believed to result in signal transduction, cytoskeletal and adhesion changes, ultimately promoting a tumor-invasive phenotype. We report here the discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of the c-Src enzyme. Special attention was directed toward finding inhibitors selective against KDR tyrosine kinase in order to ensure that the in vivo profile of a… CONTINUE READING

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