Synthesis, characterization, in vitro SAR and in vivo evaluation of N,N′bisnaphthylmethyl 2-alkyl substituted imidazolium salts against NSCLC

详细信息    查看全文

• 作者：Michael A. DeBord^a ; Marie R. Southerland^a ; Patrick O. Wagers^a ; Kristin M. Tiemann^b ; Nikki K. Robishaw^a ; Kyle T. Whiddon^a ; Michael C. Konopka^a ; Claire A. Tessier^a ; Leah P. Shriver^a ; ^c ; Sailaja Paruchuri^a ; David A. Hunstad^b ; Matthew J. Panzner^a ; ; Wiley J. Youngs^a ; ^{youngs@uakron.edu}
• 关键词：NCI ; National Cancer Institute ; IC50 ; inhibitory concentration 50% ; NSCLC ; non-small cell lung cancer ; IC23 ; 4 ; 5-dichloro-1 ; 3-bis(naphthalen-2-ylmethyl)imidazolium bromide ; MTT ; 3-(4 ; 5-dimethylthiazol-2-yl)-2 ; 5-diphenyltetrazolium bromide ; CD ; cyclodextrin ; 2-HPβCD ; 2-hydroxypropyl-β-cyclodextrin ; FDA ; Food and Drug Administration ; PS ; phosphatidylserine ; PI ; propidium iodide ; FID ; fluorescent interacalator displacement ; CT-DNA ; calf thymus DNA ; DTP ; Developmental Therapeutics Program ; IP ; intra
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：764-775
• 全文大小：3099 K
• 卷排序：27

文摘

A series of N,N′-bisnaphthylmethyl-2-alkyl imidazolium salts was synthesized. Compounds were characterized by 1H and 13C NMR and X-ray crystallography. All compounds reported have high anti-cancer activity comparable to cisplatin. NCI-60 cell line one-dose and five-dose assays. Mechanism of action studies and in vivo toxicity study.