Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

@article{Smaill2016TyrosineKI,
  title={Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.},
  author={Jeff B Smaill and Andrea J. Gonzales and Julie Ann Spicer and Helen Tsenwhei Lee and Jessica Elizabeth Reed and Karen Elaine Sexton and Irene W. Althaus and Tong Zhu and Shannon L. Black and Adrian Blaser and William A. Denny and Paul Anthony Ellis and Stephen A. Fakhoury and Patricia J. Harvey and Ken Hook and Florence O. McCarthy and Brian Desmond Palmer and F. Rivault and Kevin Matthew Schlosser and Teresa Ann Ellis and Andrew M Thompson and Erin Trachet and Roy Thomas Winters and Haile Tecle and Alexander Bridges},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 17},
  pages={
          8103-24
        }
}
Structure-activity relationships for inhibition of erbB1, erbB2, and erbB4 were determined for a series of quinazoline- and pyrido[3,4-d]pyrimidine-based analogues of the irreversible pan-erbB inhibitor, canertinib. Cyclic amine bearing crotonamides were determined to provide rapid inhibition of cellular erbB1 autophosphorylation and good metabolic stability in liver microsome and hepatocyte assays. The influence of 4-anilino substitution on pan-erbB inhibitory potency was investigated. Several… CONTINUE READING
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