Disodium Phosphate of Norcantharidin Analogues: Design, Synthesis and their Anticancer Evaluation

To design and synthesize disodium phosphate of novel norcanthridin analogues. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumour cell lines: SMMC-7721, SGC7901, ECA109, A549 and MCF-7 producing IC50 values from 0.15 μM to >50 μM. Compounds 6 and 17 showed potency for the treatment of mammary adenocarcinoma, with IC50 value to MCF-7 cell line comparable to that of cantharidin, which proves that the phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.