Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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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)
  • Received : 2011.09.28
  • Accepted : 2011.12.26
  • Published : 2012.04.20
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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.

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References

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