Synthesis and screening of novel inositol phosphonate derivatives for anticancer functions in vitro  

作　　者：Wen-Bin Chen Jian-Bing Liu Dao-Lei Dou Fan-Bo Song Lu-Yuan Li Zhen Xi 

机构地区：[1]State Key Laboratory of Elemento-Organic Chemistry,Department of Chemical Biology,Nankai University [2]State Key Laboratory of Medicinal Chemical Biology,College of Pharmacy,Nankai University

出　　处：《Chinese Chemical Letters》2015年第3期329-333,共5页中国化学快报（英文版）

基　　金：financially supported by Tianjin Municipal Natural Science Foundation (Key Program No.12JCZDJC22000);Ministry of Science and Technology of China (Nos.2010CB126102,2011BAE06B05)

摘　　要：Phosphonates have been frequently used as suitable isosteric and isoelectronic replacements for biologically important phosphates in the development of drugs or drug candidates because of their stability toward the action of phosphatases and other enzymes.In this paper,12 mono-phosphonate inositol compounds were prepared with phosphonate instead of phosphate by two kinds of strategies,nucleophilic substitution and Arbuzov rearrangement,respectively.All compounds were evaluated in vitro for their activity against non-small cell lung cancer（NSCLC） cell line A549.Two compounds（3ac and 3bb） exhibited good antitumor activity at 10 mg/mL.Phosphonates have been frequently used as suitable isosteric and isoelectronic replacements for biologically important phosphates in the development of drugs or drug candidates because of their stability toward the action of phosphatases and other enzymes.In this paper,12 mono-phosphonate inositol compounds were prepared with phosphonate instead of phosphate by two kinds of strategies,nucleophilic substitution and Arbuzov rearrangement,respectively.All compounds were evaluated in vitro for their activity against non-small cell lung cancer（NSCLC） cell line A549.Two compounds（3ac and 3bb） exhibited good antitumor activity at 10 mg/mL.

关 键 词：phosphonate inositol toward anticancer screening instead biologically antitumor dissolved hydroxyl 

分 类 号：O627.51[理学—有机化学] TQ460.1[理学—化学]