Article
Synthesis, biological evaluation and molecular docking of novel 5-phenyl-1H-pyrazol derivatives as potential BRAF(V600E) inhibitors.
Organic & biomolecular chemistry - 7 Oct 2013
Dong Jing-Jun, Li Qing-Shan, Wang Shu-Fu, Li Cui-Yun, Zhao Xin, Qiu Han-Yue, Zhao Meng-Yue, Zhu Hai-Liang
Abstract excerpt
The RAF-MEK-ERK cascade appears to be intimately involved in the regulation of cell cycle progression and apoptosis. The BRAF(V600E) mutant results in constitutive activation of the ERK pathway, which can lead to cellular growth dysregulation. A series of 5-phenyl-1H-pyrazol derivatives (3a-5e) have been designed and synthesized, and their biological activities were evaluated as potential BRAF(V600E) inhibitors....
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