Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose) polymerase inhibitors
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.
Gangloff, Anthony R.,Brown, Jason,De Jong, Ron,Dougan, Douglas R.,Grimshaw, Charles E.,Hixon, Mark,Jennings, Andy,Kamran, Ruhi,Kiryanov, Andre,O'Connell, Shawn,Taylor, Ewan,Vu, Phong
p. 4501 - 4505
(2013/08/15)
POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds,
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Page/Page column 156-157
(2010/11/04)
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