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

被引：92

作者：

Carmi, Caterina

Cavazzoni, Andrea

Zuliani, Valentina

Lodola, Alessio

Bordi, Fabrizio

Plazzi, Pier Vincenzo

Alfieri, Roberta R.

Petronini, Pier Giorgio

Mor, Marco

机构：

[1] Univ Parma, Dipartimento Farmaceut, I-43100 Parma, Italy

[2] Univ Parma, Dipartimento Med Sperimentale, Sez Patol Mol & Immunol, I-43100 Parma, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

hydantoin; EGFR; tyrosine kinase; antiproliferative activity; antitumor; HYDANTOINS; EXPRESSION;

D O I：

10.1016/j.bmcl.2006.05.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

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页码：4021 / 4025

页数：5

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