Bioorganic and Medicinal Chemistry Letters p. 4501 - 4505 (2013)
Update date:2022-08-03
Topics:
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
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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