Synthesis and screening of novel inositol phosphonate derivatives for anticancer functions in vitro |
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| Authors: | Wen-Bin Chen Jian-Bing Liu Dao-Lei Dou Fan-Bo Song Lu-Yuan Li Zhen Xi |
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| Institution: | a State Key Laboratory of Elemento-Organic Chemistry, Department of Chemical Biology, Nankai University, Tianjin 300071, China;
b State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Nankai University, Tianjin 300071, China |
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| Abstract: | 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. |
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| Keywords: | Inositol phosphonates Anticancer Non-small cell lung cancer Nucleophilic substitution Arbuzov rearrangement |
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