Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.

Bioorg Med Chem Lett

GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA.

Published: January 2004

A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC(50) values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.

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http://dx.doi.org/10.1016/j.bmcl.2003.10.010DOI Listing

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