Synthesis, anti-proliferative activity, SAR study, and preliminary in vivo toxicity study of substituted N,N′-bis(arylmethyl)benzimidazolium salts against a panel of non-small cell lung cancer cell lines

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• 作者：Kerri L. Shelton^a ; Michael A. DeBord^a ; Patrick O. Wagers ; Marie R. Southerland ; Travis M. Williams ; Nikki K. Robishaw ; Leah P. Shriver ; Claire A. Tessier ; Matthew J. Panzner ; Wiley J. Youngs ; ^{youngs@uakron.edu}
• 关键词：NCI ; National Cancer Institute ; IC50 ; inhibitory concentration 50% ; NSCLC ; non-small cell lung cancer ; MTT ; 3-(4 ; 5-dimethylthiazol-2-yl)-2 ; 5-diphenyltetrazolium bromide ; SAR ; structure-activity relationship ; GI50 ; growth inhibition 50% ; TGI ; total growth inhibition ; LC50 ; lethal concentration 50% ; DTP ; Developmental Therapeutics Program ; 2-HPβCD ; 2-hydropropyl-β-cyclodextrin
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：25
• 期：1
• 页码：421-439
• 全文大小：2825 K
• 卷排序：25

文摘

Hydrophobic and hydrophilic benzimidazolium salts were synthesized/characterized. Benzimidazolium salts were tested for their anti-cancer properties. Lipophilic benzimidazolium salts have higher anti-cancer activity. NCI’s DTP tested 21 compounds in the NCI-60 human tumor cell line screen.