当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2.

Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2.

Abstract：

:EGFR and VEGFR-2 are involved in pathological disorders and the progression of different kinds of tumors, the combined blockade of EGFR and VEGFR signaling pathways appears to be an attractive approach to cancer therapy. In this work, a series of 4-anilinoquinazoline derivatives containing substituted diaryl urea or glycine methyl ester moiety were designed and identified as EGFR and VEGFR-2 dual inhibitors. Compounds 19i, 19j and 19l exhibited the most potent inhibitory activities against EGFR (IC50 = 1 nM, 78 nM and 51 nM, respectively) and VEGFR-2 (IC50 = 79 nM, 14 nM and 14 nM, respectively), they showed good antiproliferative activities as well. Molecular docking established the interaction of 19i with the DFG-out conformation of VEGFR-2, suggesting that they might be type II kinase inhibitors.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Zhang HQ,Gong FH,Ye JQ,Zhang C,Yue XH,Li CG,Xu YG,Sun LP

doi

10.1016/j.ejmech.2016.09.039

subject

Has Abstract

pub_date

2017-01-05 00:00:00

pages

245-254

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30769-3

journal_volume

125

pub_type

杂志文章

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