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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 2
BKCSDE 33(2)
February 20, 2012 

Synthesis of 1,6-Disubstituted 4,5,6,7-Tetrahydropyrazolo[3,4-c]pyridin-7-one Derivatives and Evaluation of Their Anticancer Activity
Vani Nelamane Devegowda, Seon Hee Seo, Ae Nim Pae, Ghilsoo Nam,*, Kyung Il Choi,*,
Tetrahydropyrazolopyridinone, 3-Aminopyrazole, Anti-proliferative activity, Anticancer drugs
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 R2 was the most potent with the IC50 values in the range as low as 0.16 to 0.40 μM.
647 - 650
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