Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors.
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.
Shi
Jianyou
J
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.
Xu
Guobin
G
Zhu
Wei
W
Ye
Haoyu
H
Yang
Shengyong
S
Luo
Youfu
Y
Han
Jing
J
Yang
Jincheng
J
Li
Rui
R
Wei
Yuquan
Y
Chen
Lijuan
L
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*
D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases