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Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.

Abstract：

:The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC(50) values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)quinazolines provided scaffolds for potent enzyme inhibition. Chiral discrimination was observed to occur in one of the 4-alkynylquinazoline derivatives with the (R)-isomer being more than 150 times as potent as the (S)-isomer.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kitano Y,Suzuki T,Kawahara E,Yamazaki T

doi

10.1016/j.bmcl.2007.08.020

subject

Has Abstract

pub_date

2007-11-01 00:00:00

pages

5863-7

issue

21

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00968-7

journal_volume

17

pub_type

杂志文章

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