Synthesis, biological evaluation and molecular docking studies of novel 2-(1, 3, 4-oxadiazol-2-ylthio)-1-phenylethanone derivatives

…, H Zhang, J Sun, Y Luo, TT Zhao, HB Gong…

Index: Zhang, Li-Rong; Liu, Zhi-Jun; Zhang, Hui; Sun, Jian; Luo, Yin; Zhao, Ting-Ting; Gong, Hai-Bin; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 11 p. 3615 - 3621

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Citation Number: 10

Abstract

In present study, a series of new 2-(1, 3, 4-oxadiazol-2-ylthio)-1-phenylethanone derivatives (6a–6x) as potential focal adhesion kinase (FAK) inhibitors were synthesized. The bioassay assays demonstrated that compound 6i showed the most potent activity, which inhibited the growth of MCF-7 and A431 cell lines with IC50 values of 140±10nM and 10±1nM, respectively. Compound 6i also exhibited significant FAK inhibitory activity (IC50= 20± ...