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Your search keyword '"Stephen Barry Stevenage Guntrip"' showing total 2 results
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2 results on '"Stephen Barry Stevenage Guntrip"'

1. Synthesis and SAR of Potent EGFR/erbB2 Dual Inhibitors

Author

Stephen Barry Stevenage Guntrip, Kathryn Smith, Stuart Cockerill, Dana E. Vanderwall, Yue-Mei Zhang, Karen Lackey, David W. Rusnak, and Edgar R. Wood

Subjects
Receptor, ErbB-2, Clinical Biochemistry, Pharmaceutical Science, Tumor cells, Biochemistry, Chemical synthesis, Structure-Activity Relationship, Growth factor receptor, Epidermal growth factor, Cell Line, Tumor, Drug Discovery, Humans, Structure–activity relationship, Enzyme Inhibitors, Kinase activity, Molecular Biology, Glycoproteins, Binding Sites, biology, Chemistry, Organic Chemistry, General Medicine, In vitro, ErbB Receptors, Enzyme inhibitor, biology.protein, Cancer research, Molecular Medicine, Signal transduction
Abstract

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.

Published
2004
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2. Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines

Author

Yu Guo, Sarva M. Tadepalli, G. Stuart Cockerill, Kathryn Smith, Edgar R. Wood, Barry R. Keith, David W. Rusnak, Robert J. Mullin, Micheal D. Gaul, Robert J. Griffin, Wilson B. Knight, Tona M. Gilmer, Karen Lackey, Stephen Barry Stevenage Guntrip, Karen Affleck, and Doris M. Murray

Subjects
Receptor, ErbB-2, Clinical Biochemistry, Transplantation, Heterologous, Pharmaceutical Science, Antineoplastic Agents, Mice, Inbred Strains, Biochemistry, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, Growth factor receptor, ErbB, In vivo, Epidermal growth factor, Cell Line, Tumor, Drug Discovery, Animals, Humans, Enzyme Inhibitors, skin and connective tissue diseases, Molecular Biology, biology, Chemistry, Organic Chemistry, Neoplasms, Experimental, In vitro, Transplantation, ErbB Receptors, Enzyme inhibitor, Cancer research, biology.protein, Quinazolines, Molecular Medicine, Female, Signal transduction
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.

Published
2003

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