21418-62-2Relevant academic research and scientific papers
Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment
Devegowda, Vani Nelamane,Hong, Jin-Ri,Cho, Sungjin,Lim, Eun Jeong,Choo, Hyunah,Keum, Gyochang,Rhim, Hyewon,Nam, Ghilsoo
, p. 4696 - 4700 (2013/08/23)
A novel series of 3-arylsulfonylamino-5,6-dihydro-6-substituted-1H- pyrazolo[3,4-c]pyridine-7-ones was designed and synthesized as 5-HT6 ligands. Among the derivatives synthesized, the lead compound, 12b, having piperidine functionality at the 6-position and (1-naphthyl)sulfonamino at the 3-position of the core structure showed the most potent 5-HT6 inhibitory activity in vitro, good stability without CYP liability, and good neuropathic pain alleviation activity in a rat animal model.
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,Seo, Seon Hee,Pae, Ae Nim,Nam, Ghilsoo,Choi, Kyung Il
scheme or table, p. 647 - 650 (2012/05/04)
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.
NOVEL 1,6-DISUBSTITUTED-3-AMINO-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[3,4-C]PYRIDIN-7-ONE COMPOUNDS AND PREPARATION THEREOF
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Page/Page column 5-6, (2012/01/13)
Provided are a novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound, a pharmaceutically acceptable salt compound thereof, a method for preparing the compound, and an anticancer pharmaceutical composition including the compound as an effective ingredient.
