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Synthesis, X-ray crystallographic analysis, and antitumor activity of N-(benzothiazole-2-yl)-1-(fluorophenyl)-O,O-dialkyl-alpha-aminophosphonates
Authors:Jin Linhong  Song Baoan  Zhang Guoping  Xu Ruiqing  Zhang Sumei  Gao Xingwen  Hu Deyu  Yang Song
Institution:Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
Abstract:Alpha-aminophosphonates containing benzothiazole and fluorine moiety, 4a-4m, were synthesized by Mannich-type addition in ionic liquid media with high yield and short reaction time. Their structures were established by IR, (1)H NMR, (13)C NMR, and elemental analysis. The X-ray crystallographic data of compounds 4j and 4m were provided. The newly synthesized compounds were evaluated for their anticancer activities against PC3, A431, A375, and Bcap37 cells in vitro by the MTT method. Compound 4c is highly effective against PC3 cells and moderate to A431 cells. Hence, further study is necessary to find out the potential antitumor activities.
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