Preparation and anticancer activity of isopimaric acid heterocyclic amide derivatives
In order to develop antitumor drugs with new molecular structure,nine heterocyclic amide compounds(Ⅱa～Ⅱi)were synthesized from natural product isopimaric acid(Ⅰ),and characterized by FTIR,1HNMR,13CNMR and TOF-MS.Data from anti-tumor performance analysis revealed that except forⅡf,all the other target compounds showed higher anti-tumor activities than the natural isopimaric acid.Especially compound isopimaric acyl-(2-aminopyrazine)amide(Ⅱd)containing pyrazine heterocycle exhibited significant cell proliferation inhibitory activity against A375 human melanoma cells,with a half maximal inhibitory concentration(IC50)of 13.34 μmol/L.Therefore,compound Ⅱd is expected for antitumor activity improvement through further structural modification and become a leading anti-tumor compound of isopimaric acid.
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