Inositol phosphates regulate important biological functions in intracellular signal transduction events. Phosphonates, because of the stability towards the action of phosphatases, were extensively used to replace phosphates. We herein reported the synthesis of inositol phosphonate analogues using myo-inositol as the starting material, and found that two of phosphonate analogues exhibited relative good cytotoxic activity against non-small cell lung cancer (NSCLC) cell line A549.