Synthesis, biological evaluation and 3D-QSAR studies of novel 4, 5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors

…, L Yan, XG Sun, R Wei, HB Gong, HL Zhu

Index: Li, Cui-Yun; Li, Qing-Shan; Yan, Li; Sun, Xiao-Guang; Wei, Ran; Gong, Hai-Bin; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 12 p. 3746 - 3755

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Citation Number: 15

Abstract

A series of novel 4, 5-dihydropyrazole derivatives containing niacinamide moiety as potential V600E mutant BRAF kinase (BRAFV600E) inhibitors were designed and synthesized. Results of the bioassays against BRAFV600E and WM266. 4 human melanoma cell line showed several compounds to be endowed potent activities with IC50 and GI50 value in low micromolar range, among which compound 27e,(5-(4-Chlorophenyl ...