摘要

A series of norcantharidin (NCTD) analogues have been synthesized by [3+2]1,3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with four nitrile oximes. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SGC-7901, HL60, Bel-7402, HO-8910, and ECA109, producing IC50 values from 0.36 mu mol/L to >100 mu mol/L. Compound 9d showed potency for the treatment of hepatoma, with IC50 value to Bel-7402 cell line comparable to that of norcantharidin.