Synthesis, biological evaluation of novel 4, 5-dihydro-2H-pyrazole 2-hydroxyphenyl derivatives as BRAF inhibitors

JJ Liu, H Zhang, J Sun, ZC Wang, YS Yang…

Index: Liu, Jia-Jia; Zhang, Hui; Sun, Juan; Wang, Zhong-Chang; Yang, Yu-Shun; Li, Dong-Dong; Zhang, Fei; Gong, Hai-Bin; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 20 p. 6089 - 6096

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Citation Number: 15

Abstract

A series of novel 4, 5-dihydropyrazole derivatives (3a–3t) containing hydroxyphenyl moiety as potential V600E mutant BRAF kinase (BRAFV600E) inhibitors were designed and synthesized. Docking simulation was performed to insert compounds 3d (1-(5-(5-chloro-2- hydroxyphenyl)-3-(p-tolyl)-4, 5-dihydro-1H-pyrazol-1-yl) ethanone) and 3m (1-(3-(4- chlorophenyl)-5-(3, 5-dibromo-2-hydroxyphenyl)-4, 5-dihydro-1H-pyrazol-1-yl) ethanone) ...