5-benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4021-5. doi: 10.1016/j.bmcl.2006.05.010. Epub 2006 May 19.


A series of 1,5-disubstituted hydantoins, whose structure was designed to interact at the ATP-binding site of EGFR, was synthesized and evaluated for inhibition of EGFR kinase activity and antiproliferative action. Some of these compounds, characterized by a 1-phenethyl and a 5-(E)-benzylidene substituent, inhibited EGFR autophosphorylation and polyGAT phosphorylation, and also inhibited the growth and proliferation of human A431 cells, which overexpress EGFR. These compounds can therefore be regarded as examples of a new scaffold for tyrosine kinase inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Cell Proliferation / drug effects*
  • ErbB Receptors / antagonists & inhibitors*
  • Humans
  • Hydantoins / chemistry
  • Hydantoins / pharmacology*
  • Models, Molecular
  • Structure-Activity Relationship


  • Hydantoins
  • ErbB Receptors