| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372279 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic & cellular activities and pharmacodynamic effects are described. Optimized analogs demonstrated inhibition of poly-ADP-ribosylation in SW620 tumor bearing nude mice through 24 h following a single dose.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors](/preview/png/1372279.png "First Page Preview: Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors")
Authors
Anthony R. Gangloff, Jason Brown, Ron de Jong, Douglas R. Dougan, Charles E. Grimshaw, Mark Hixon, Andy Jennings, Ruhi Kamran, Andre Kiryanov, Shawn O’Connell, Ewan Taylor, Phong Vu,