Abstract
Twenty-one 1, 2, 3-triazole-linked norcantharidin analogues have been synthesized by the efficient [3+2]1, 3- dipolar cycloaddition reaction of norcantharidin derivatives with three organic azides. All analogues have been screened for their antiproliferative activity against a panel of tumor cell lines: KB, SMMC-7721, SGC7901, ECA109, HO8910 and K562. Compound 8e showed potency for the treatment of hepatoma, with GI50 value (19.0±0.2μM) to SMMC-7721 cell line comparable to that of cantharidin (GI50 value =33.2±0.3μM).
Keywords: 1, 2, 3-Triazole-linked, Cantharidin, Norcantharidin analogues, Cycloaddition, Tumor cell lines, Growth inhibition
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