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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 4
BKCSDE 33(4)
April 20, 2012 

 
Title
Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors
Author
Sunkyung Lee,* Kyu Yang Yi, Byung Ho Lee, Kwang Seok Oh
Keywords
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor, Benzofuran-7-carboxamide, Nicotinamide, Anticancer, Ischemic disease
Abstract
Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]- benzofuran-7-carboxamide (42) was the most potent as an IC50 value of 40 nM among those.
Page
1147 - 1153
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