Title of article
Discovery and Biological Evaluation of Potent Dual ErbB-2/EGFR Tyrosine Kinase Inhibitors: 6-Thiazolylquinazolines
Author/Authors
Micheal D. Gaul، نويسنده , , Yu Guo، نويسنده , , Karen Affleck، نويسنده , , G. Stuart Cockerill، نويسنده , , Tona M. Gilmer، نويسنده , , Robert J. Griffin، نويسنده , , Stephen Guntrip، نويسنده , , Barry R. Keith، نويسنده , , Wilson B. Knight، نويسنده , , Robert J. Mullin، نويسنده , , Doris M. Murray، نويسنده , , David W. Rusnak، نويسنده , , Kathryn Smith، نويسنده , , Sarva Tadepalli، نويسنده , , Edgar R. Wood، نويسنده , , Karen Lackey، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
637
To page
640
Abstract
We have identified a novel class of 6-thiazolylquinazolines as potent and selective inhibitors of both ErbB-2 and EGFR tyrosine kinase activity, with IC50 values in the nanomolar range. These compounds inhibited the growth of both EGFR (HN5) and ErbB-2 (BT474) over-expressing human tumor cell lines in vitro. Using xenograft models of the same cell lines, we found that the compounds given orally inhibited in vivo tumor growth significantly compared with control animals.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792982
Link To Document