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http://dx.doi.org/10.5012/bkcs.2012.33.2.647

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)
Publication Information
Bulletin of the Korean Chemical Society / v.33, no.2, 2012 , pp. 647-650 More about this Journal
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 $0.40{\mu}M$.
Keywords
Tetrahydropyrazolopyridinone; 3-Aminopyrazole; Anti-proliferative activity; Anticancer drugs;
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