| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10598166 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion assay. BMS-316810 (9e), a 0.7Â nM FT inhibitor, was orally-active in a nude mouse tumor allograft efficacy study.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Louis J. Lombardo, Amy Camuso, John Clark, Krista Fager, Johnni Gullo-Brown, John T. Hunt, Ivan Inigo, David Kan, Barry Koplowitz, Francis Lee, Kelly McGlinchey, Ligang Qian, Carolyn Ricca, George Rovnyak, Sarah Traeger, John Tokarski, David K. Williams,