Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365391 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Starting from initial lead 1 containing a basic 5-substituent, optimisation of the glycolamide-derived neutral 5-substituent led to potent inhibitors of erbB2 with good pharmacokinetics. Representative compounds 19 and 21 inhibited phosphorylation of erbB2 in a mouse BT474C xenograft model after oral administration.
Graphical abstractStarting from initial lead 1 containing a basic 5-substituent, optimisation of the glycolamide-derived neutral 5-substituent led to potent inhibitors of erbB2 with good pharmacokinetics. Representative compounds 19 and 21 inhibited phosphorylation of erbB2 in a mouse BT474C xenograft model after oral administration.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Bernard Barlaam, Peter Ballard, Robert H. Bradbury, Richard Ducray, Hervé Germain, D. Mark Hickinson, Kevin Hudson, Jason G. Kettle, Teresa Klinowska, Françoise Magnien, Donald J. Ogilvie, Annie Olivier, Stuart E. Pearson, James S. Scott, Abid Suleman,