4-anilino-3-quinolinecarbonitriles: an emerging class of kinase inhibitors.

  title={4-anilino-3-quinolinecarbonitriles: an emerging class of kinase inhibitors.},
  author={Diane H Boschelli},
  journal={Current topics in medicinal chemistry},
  volume={2 9},
The first potent selective small molecule inhibitor of a protein kinase was reported in 1994 by Parke-Davis. PD-153035, 4-(3-bromoanilino)-6,7-dimethoxyquinazoline, is an ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFr), with no appreciable inhibitory activity against several other kinases. Subsequent structural elaboration of PD-153035 led to several 4-anilinoquinazolines that are currently in various stages of clinical trials for the treatment of kinase… CONTINUE READING