Synthesis of 1,6-Disubstituted 4,5,6,7-Tetrahydropyrazolo[3,4-c]pyridin-7-one Derivatives and Evaluation of Their Anticancer Activity

Bulletin of the Korean chemical society

Vani Nelamane Devegowda¹  Ae Nim Pae¹  Seon Hee Seo¹  Kyung Il Choi¹  Ghilsoo Nam¹ 

关键词: Tetrahydropyrazolopyridinone;    3-Aminopyrazole;    Anti-proliferative activity;    Anticancer drugs;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown