title: Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors.
abstract: Two series of 3-aminopyrazole compounds including 24 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and 16 pyrazolo[3,4-b]pyridines were synthesized and evaluated against HCT116, A549, and A2780 tumor cell lines. Among them, three compounds were found to have the ideal anti-proliferative activities in vitro. Docking experiments showed that the novel pyrazolo[3,4-b]pyridines share the similar interaction mode with Aurora-A kinase as PHA739358.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu, Sichuan 610041, PR China.
authors.forename: Jianyou
authors.initials: J
authors.lastname: Shi
authors.forename: Guobin
authors.initials: G
authors.lastname: Xu
authors.forename: Wei
authors.initials: W
authors.lastname: Zhu
authors.forename: Haoyu
authors.initials: H
authors.lastname: Ye
authors.forename: Shengyong
authors.initials: S
authors.lastname: Yang
authors.forename: Youfu
authors.initials: Y
authors.lastname: Luo
authors.forename: Jing
authors.initials: J
authors.lastname: Han
authors.forename: Jincheng
authors.initials: J
authors.lastname: Yang
authors.forename: Rui
authors.initials: R
authors.lastname: Li
authors.forename: Yuquan
authors.initials: Y
authors.lastname: Wei
authors.forename: Lijuan
authors.initials: L
authors.lastname: Chen
mesh_terms: D064127:Aurora Kinases; D045744:Cell Line, Tumor; D006801:Humans; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases