Design, modification and 3D QSAR studies of novel 2, 3-dihydrobenzo [b][1, 4] dioxin-containing 4, 5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase

…, S Sun, YB Zhang, XL Wang, F Zhang, JF Tang…

Index: Yang, Yu-Shun; Li, Qing-Shan; Sun, Shuai; Zhang, Yan-Bin; Wang, Xiao-Liang; Zhang, Fei; Tang, Jian-Feng; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 20 p. 6048 - 6058

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Citation Number: 12

Abstract

Two series of novel 2, 3-dihydrobenzo [b][1, 4] dioxin-containing 4, 5-dihydro-1H-pyrazole derivatives C1–C15 and D1–D15 have been synthesized and evaluated for their B-Raf inhibitory and anti-proliferation activities. Compound C14 ((3-(4-bromophenyl)-5-(2- fluorophenyl)-4, 5-dihydro-1H-pyrazol-1-yl)(2, 3-dihydrobenzo [b][1, 4] dioxin-6-yl) methanone) showed the most potent biological activity against B-RafV600E (IC50= 0.11 ...