Synthesis and biological evaluation of nitric oxide-releasing sixalkoxyl biphenyl derivatives as anticancer agents  

作　　者：Xiang Wen Kong Yi Hua Zhang Li Dai Hui Ji Yi Sheng Lai Si Xun Peng 

机构地区：[1]Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China [2]Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, China

出　　处：《Chinese Chemical Letters》2008年第2期149-152,共4页中国化学快报（英文版）

摘　　要：A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against HepG2 cells in vitro were evaluated by MTT method. It was found that 14c, 14d, 14f, 14i, 14j and 14k showed more potent cytotoxic activities than control 5-fluorouracil. NO release assay of target compounds indicated that the maximum amount of NO released by most active compounds 14c and 14j was about 6 × 10^-2 μmol/L, whereas 14a and 14h with very weak activity only released NO of 1 × 10^-2 μmol/L.A series of novel nitric oxide-donating sixalkoxyl biphenyl derivatives （14a-1） were synthesized by coupling furoxan with alkoxyl biphenyl skeleton using amino acids as the spacers, and their cytotoxicity against HepG2 cells in vitro were evaluated by MTT method. It was found that 14c, 14d, 14f, 14i, 14j and 14k showed more potent cytotoxic activities than control 5-fluorouracil. NO release assay of target compounds indicated that the maximum amount of NO released by most active compounds 14c and 14j was about 6 × 10^-2 μmol/L, whereas 14a and 14h with very weak activity only released NO of 1 × 10^-2 μmol/L.

关 键 词：Nitric oxide-donating sixalkoxyl biphenyl derivatives FUROXAN CYTOTOXICITY 

分 类 号：TQ17[化学工程—硅酸盐工业]