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 ac...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.展开更多
基金financially supported by Tianjin Municipal Natural Science Foundation (Key Program No.12JCZDJC22000)Ministry of Science and Technology of China (Nos.2010CB126102,2011BAE06B05)
文摘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.
