Optimization of gefitinib analogues with potent anticancer activity.

  title={Optimization of gefitinib analogues with potent anticancer activity.},
  author={Kai-Hao Yin and Yi-Han Hsieh and Rohidas S Sulake and Su-Pei Wang and Jui-I Chao and Chinpiao Chen},
  journal={Bioorganic & medicinal chemistry letters},
  volume={24 22},
The interactions of gefitinib (Iressa) in EGFR are hydrogen bonding and van der Waals forces through quinazoline and aniline rings. However the morpholino group of gefitinib is poorly ordered due to its weak electron density. A series of novel piperazino analogues of gefitinib where morpholino group substituted with various piperazino groups were designed… CONTINUE READING