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

Bioorganic & Medicinal Chemistry Letters
2006.0

Abstract

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.

Knowledge Graph

Similar Paper

5-Benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity
Bioorganic & Medicinal Chemistry Letters 2006.0
5-Benzylidene-hydantoins: Synthesis and antiproliferative activity on A549 lung cancer cell line
European Journal of Medicinal Chemistry 2009.0
Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase
Bioorganic & Medicinal Chemistry Letters 2004.0
Discovery of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-ones as novel EGFR inhibitor by scaffold hopping
Bioorganic & Medicinal Chemistry 2013.0
Combination of 4-anilinoquinazoline and rhodanine as novel epidermal growth factor receptor tyrosine kinase inhibitors
Bioorganic & Medicinal Chemistry 2015.0
Design, synthesis and biological evaluation of novel 3,4-dihydro-2H-[1,4]oxazino [2,3-f]quinazolin derivatives as EGFR-TKIs
Bioorganic & Medicinal Chemistry Letters 2023.0
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors
Bioorganic & Medicinal Chemistry 2020.0
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors
Journal of Medicinal Chemistry 1989.0
Novel 4-arylaminoquinazoline derivatives with ( E )-propen-1-yl moiety as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells
European Journal of Medicinal Chemistry 2017.0
Schiff’s base derivatives bearing nitroimidazole moiety: New class of antibacterial, anticancer agents and potential EGFR tyrosine kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2013.0