| Autor: |
Hubbard RD; GlaxoSmithKline Research & Development, Research Triangle Park, NC 27709-3398, USA., Dickerson SH, Emerson HK, Griffin RJ, Reno MJ, Hornberger KR, Rusnak DW, Wood ER, Uehling DE, Waterson AG |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Nov 01; Vol. 18 (21), pp. 5738-40. Date of Electronic Publication: 2008 Sep 27. |
| DOI: |
10.1016/j.bmcl.2008.09.090 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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