Design, synthesis and biological evaluation of novel 1,3,4-trisubstituted pyrazole derivatives as potential chemotherapeutic agents for hepatocellular carcinoma

2018 ◽  
Vol 78 ◽  
pp. 149-157 ◽  
Author(s):  
Marwa F. Harras ◽  
Rehab Sabour
Keyword(s):  
Hepatocellular Carcinoma ◽  
Biological Evaluation ◽  
Chemotherapeutic Agents ◽  
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 new 4-thiazolidinone derivatives substituted with benzimidazole ring as potential chemotherapeutic agents

2012 ◽  
Vol 22 (2) ◽  
pp. 707-725 ◽  
Author(s):  
Georgina N. Masoud ◽  
Amal M. Youssef ◽  
Magdy M. Abdel Khalek ◽  
Abeer E. Abdel Wahab ◽  
Ibrahim M. Labouta ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Chemotherapeutic Agents ◽  
Benzimidazole Ring ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation

2016 ◽  
Vol 88 (4) ◽  
pp. 592-598 ◽  
Author(s):  
Long-Wang Chen ◽  
Peng-Fei Wang ◽  
Dan-Jie Tang ◽  
Xiang-Xiang Tao ◽  
Ruo-Jun Man ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Trna Synthetase ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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