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 IC 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.
Keywords: Norcantharidin analogues, Phosphorylation, Anticancer evaluation, Solubility
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