| Literature DB >> 12639547 |
Micheal D Gaul1, Yu Guo, Karen Affleck, G Stuart Cockerill, Tona M Gilmer, Robert J Griffin, Stephen Guntrip, Barry R Keith, Wilson B Knight, Robert J Mullin, Doris M Murray, David W Rusnak, Kathryn Smith, Sarva Tadepalli, Edgar R Wood, Karen Lackey.
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 IC(50) 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.Entities:
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Year: 2003 PMID： 12639547 DOI： 10.1016/s0960-894x(02)01047-8
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823