Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis of 1,6-Disubstituted 4,5,6,7-Tetrahydropyrazolo[3,4-c]pyridin-7-one Derivatives and Evaluation of Their Anticancer Activity

  • Devegowda, Vani Nelamane (Life/Health Division, Korea Institute of Science and Technology) ;
  • Seo, Seon-Hee (Life/Health Division, Korea Institute of Science and Technology) ;
  • Pae, Ae Nim (Life/Health Division, Korea Institute of Science and Technology) ;
  • Nam, Ghil-Soo (Life/Health Division, Korea Institute of Science and Technology) ;
  • Choi, Kyung-Il (Life/Health Division, Korea Institute of Science and Technology)
  • Received : 2011.08.23
  • Accepted : 2011.10.24
  • Published : 2012.02.20
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Abstract

Promising anticancer compounds of the type 1,6-disubstituted 4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-7-ones were identified. The target compounds were readily synthesized in a large scale via a sequence of reactions starting from the commercially available primary amines. Their in vitro anti-proliferative activity has been evaluated on prostate (DU-145), colon (HT-29 and HCT-116) and melanoma (A375P) human cancer cell lines. The relationships between the structure and the anticancer activity, covering all tested cancer cell lines, revealed that the compound 5c with 2,4-dimethylphenyl substituent at $R^2$ was the most potent with the $IC_{50}$ values in the range as low as 0.16 to $0.40{\mu}M$.

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