Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 16, Pages 4501-4505Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.055
Keywords
Poly(ADP-ribose)polymerase inhibitors; PARP-1; Structure-based drug design; 1,4-Benzoxazin-3-one; Chemopotentiation
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Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic 82 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. (c) 2013 Elsevier Ltd. All rights reserved.
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