Discovery of boron-conjugated 4-anilinoquinazoline as a prolonged inhibitor of EGFR tyrosine kinase.

@article{Ban2009DiscoveryOB,
  title={Discovery of boron-conjugated 4-anilinoquinazoline as a prolonged inhibitor of EGFR tyrosine kinase.},
  author={Hyun Seung Ban and Taikou Usui and Wataru Nabeyama and Hidetoshi Morita and Kaori Fukuzawa and Hiroyuki Nakamura},
  journal={Organic & biomolecular chemistry},
  year={2009},
  volume={7 21},
  pages={4415-27}
}
Boron-conjugated 4-anilinoquinazolines were designed and synthesized as inhibitors of EGFR tyrosine kinase with possible covalent bond interactions between the boron atom and the nucleophilic groups of the EGFR kinase domain. Among the compounds synthesized, compounds 6c, 7b, and 7d reduced the EGF-mediated phosphorylation of EGFR tyrosine kinase and its downstream kinases including ERK and Akt in A431 cells. The cell growth was inhibited by these compounds through arrest of G1 cell cycle… CONTINUE READING
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