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Kyu Yang Yi, Byung Ho Lee, and Kwang Seok OhBio-Organic Science Division, Korea Research Institute of Chemical Technology, P.O. Box 107, Daejeon 305-600, Korea*E-mail: leesk@krict.re.kr Received September 28, 2011, Accepted December 26, 2011Benzofuran-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 sub-stituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluatedto 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 IC

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