Design, synthesis and biological evaluation of pyrazole derivatives as potential multi-kinase inhibitors in hepatocellular carcinoma

2012 ◽  
Vol 48 ◽  
pp. 391-401 ◽  
Author(s):  
Elena Strocchi ◽  
Francesca Fornari ◽  
Manuela Minguzzi ◽  
Laura Gramantieri ◽  
Maddalena Milazzo ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, and Biological Evaluation of Pyrano[2,3-c]-pyrazole–Based RalA Inhibitors Against Hepatocellular Carcinoma

2021 ◽  
Vol 9 ◽  
Author(s):  
Yuting Wang ◽  
Mingyao He ◽  
Xiang Li ◽  
Jinlong Chai ◽  
Qinglin Jiang ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cell Proliferation ◽  
Cellular Proliferation ◽  
Biological Evaluation ◽  
Small Gtpases ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Tumor Progress ◽  
Proliferation Assays ◽  
Synthesis And Biological Evaluation

The activation of Ras small GTPases, including RalA and RalB, plays an important role in carcinogenesis, tumor progress, and metastasis. In the current study, we report the discovery of a series of 6-sulfonylamide-pyrano [2,3-c]-pyrazole derivatives as novel RalA inhibitors. ELISA-based biochemical assay results indicated that compounds 4k–4r suppressed RalA/B binding capacities to their substrates. Cellular proliferation assays indicated that these RalA inhibitors potently inhibited the proliferation of HCC cell lines, including HepG2, SMMC-7721, Hep3B, and Huh-7 cells. Among the evaluated compounds, 4p displayed good inhibitory capacities on RalA (IC50 = 0.22 μM) and HepG2 cells (IC50 = 2.28 μM). Overall, our results suggested that a novel small-molecule RalA inhibitor with a 6-sulfonylamide-pyrano [2, 3-c]-pyrazole scaffold suppressed autophagy and cell proliferation in hepatocellular carcinoma, and that it has potential for HCC-targeted therapy.

Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAFV600E inhibitors

2014 ◽  
Vol 22 (21) ◽  
pp. 6201-6208 ◽  
Author(s):  
Shu-Fu Wang ◽  
Yin-Ling Zhu ◽  
Ping-Ting Zhu ◽  
Jigar A. Makawana ◽  
Ya-Liang Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation

2020 ◽  
Vol 30 (16) ◽  
pp. 127327
Author(s):  
Zhicheng Su ◽  
Tingyuan Yang ◽  
Jie Wang ◽  
Mengzhen Lai ◽  
Linjiang Tong ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Egfr Kinase

scholarly journals Design, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors

2011 ◽  
Vol 54 (20) ◽  
pp. 7427-7431 ◽  
Author(s):  
Christine Dyrager ◽  
Linda Nilsson Möllers ◽  
Linda Karlsson Kjäll ◽  
John Patrick Alao ◽  
Peter Dinér ◽  
...  
Keyword(s):  
Map Kinase ◽  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
P38 Map Kinase ◽  
Design Synthesis ◽  
P38 Map Kinase Inhibitors ◽  
Synthesis And Biological Evaluation
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