Imide cantharidin derivatives: Synthesis and HBV-DNA inhibitory properties.

Cantharidin and its analogs are potent serine/threonine protein phosphatase inhibitors with rare reports on inhibiting expression of Hepatitis B virus (HBV) DNA. Five imide cantharidin derivatives were synthesized, and their properties were studied. The inhibition efficiency was determined, and preliminary studies on the structure-activity relationships were conducted. The results indicated that the compounds characterized by low Log P values and the cantharidin moieties containing nitrogen exhibited low cytotoxicity and helped inhibit the expression of HBV DNA. Compound 2 and the non-cytotoxic compound 3 significantly inhibited the expression of HBV DNA. The IC50 values recorded for both compounds were 2.0±1.2 and 19.2±2.0 nM, respectively. [ABSTRACT FROM AUTHOR]