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.

5-Benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity / Carmi, Caterina; Cavazzoni, Andrea; Zuliani, Valentina; Lodola, Alessio; Bordi, Fabrizio; Plazzi, Pier Vincenzo; Alfieri, Roberta; Petronini, Pier Giorgio; Mor, Marco. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 16:(2006), pp. 4021-4025. [10.1016/j.bmcl.2006.05.010]

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

CARMI, Caterina;CAVAZZONI, Andrea;ZULIANI, Valentina;LODOLA, Alessio;BORDI, Fabrizio;PLAZZI, Pier Vincenzo;ALFIERI, Roberta;PETRONINI, Pier Giorgio;MOR, Marco
2006-01-01

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.
5-Benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity / Carmi, Caterina; Cavazzoni, Andrea; Zuliani, Valentina; Lodola, Alessio; Bordi, Fabrizio; Plazzi, Pier Vincenzo; Alfieri, Roberta; Petronini, Pier Giorgio; Mor, Marco. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 16:(2006), pp. 4021-4025. [10.1016/j.bmcl.2006.05.010]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2295790
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