title: 5-benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity.
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.
authors.affiliation: Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G. P. Usberti 27/A, I-43100 Parma, Italy.
authors.forename: Caterina
authors.initials: C
authors.lastname: Carmi
authors.forename: Andrea
authors.initials: A
authors.lastname: Cavazzoni
authors.forename: Valentina
authors.initials: V
authors.lastname: Zuliani
authors.forename: Alessio
authors.initials: A
authors.lastname: Lodola
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Bordi
authors.forename: Pier Vincenzo
authors.initials: PV
authors.lastname: Plazzi
authors.forename: Roberta R
authors.initials: RR
authors.lastname: Alfieri
authors.forename: Pier Giorgio
authors.initials: PG
authors.lastname: Petronini
authors.forename: Marco
authors.initials: M
authors.lastname: Mor
mesh_terms: D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D006827:Hydantoins / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D013329:Structure-Activity Relationship
chemical_list: D006827:Hydantoins; D066246:ErbB Receptors