[KSCI] Korea Science Citation Index Service

http://dx.doi.org/10.5012/bkcs.2012.33.4.1147

Studies on Benzofuran-7-carboxamides as Poly(ADP-ribose) Polymerase-1 (PARP-1) Inhibitors

Lee, Sun-Kyung (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)
Yi, Kyu-Yang (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)
Lee, Byung-Ho (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)
Oh, Kwang-Seok (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)

Publication Information

Bulletin of the Korean Chemical Society / v.33, no.4, 2012 , pp. 1147-1153 More about this Journal

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.

Keywords

Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor; Benzofuran-7-carboxamide; Nicotinamide; Anticancer; Ischemic disease;

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