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

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 μg/mL.

Graphical abstractTwelve mono-phosphonate inositol compounds were prepared, and two of them (3ac and 3bb) exhibited good antitumor activity against non-small cell lung cancer (NSCLC) cell line A549 at 10 μg/mL.Figure optionsDownload full-size imageDownload as PowerPoint slide