Title of article
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines
Author/Authors
Robert D. Hubbard، نويسنده , , Scott H. Dickerson، نويسنده , , Holly K. Emerson، نويسنده , , Robert J. Griffin، نويسنده , , Michael J. Reno، نويسنده , , Keith R. Hornberger، نويسنده , , David W. Rusnak، نويسنده , , Edgar R. Wood، نويسنده , , David E. Uehling، نويسنده , , Alex G. Waterson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
3
From page
5738
To page
5740
Abstract
A novel class of substituted pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines has been identified that are potent and selective inhibitors of both EGFR/ErbB-2 receptor tyrosine kinases. The inhibitors are found to display a range of enzyme and cellular potency and also to display a varying level of covalent modification of the kinase targets. Selected molecules, including compound 15h, were found to be potent in enzymatic and cellular assays while also demonstrating exposure in the mouse from an oral dose.
Keywords
2-d]pyrimidines , epidermal growth factor receptor , EGFR , ErbB-2 , inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800098
Link To Document