| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365046 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Using a cell-based assay, we have identified a new series of Notch-sparing γ-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved γ-secretase inhibitory potency and Notch-sparing selectivity.
Graphical abstractLead optimization studies of Notch-sparing GSI 2a led to the discovery of analog 8e with improved γ-secretase inhibitory potency and Notch-sparing selectivity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Anthony Kreft, Boyd Harrison, Suzan Aschmies, Kevin Atchison, David Casebier, Derek C. Cole, George Diamantidis, John Ellingboe, Diane Hauze, Yun Hu, Donna Huryn, Mei Jin, Dennis Kubrak, Peimin Lu, Joseph Lundquist, Charles Mann, Robert Martone,