Synthesis and Anti-angiogenesis Activities of Ursolic Acid Derivatives

Twenty-four derivatives of ursolic acid modified at C3 and C28 were designed and synthesized for the investigation of the structure-activity relationship of ursolic acid(1) against angiogenesis.All the com-pounds were characterized by 1H NMR,13C NMR,MS and HR-MS.HUVEC was used as an angiogenesis tar-get cell and A549,Bel-7402 and MCF-7 were as cancer target cells and the antiproliferative activity was as-sayed by MTT method.The results show that compounds 5,9,12e and 14e possess the selectively antiprolif-erative activity of HUVEC,meanwhile,compounds 12a and 13h are more active than compound 1 against the proliferation of HUVEC.Therefore,it is possible that more potent and selective angiogenesis inhibitors of ur-solic acid derivatives could be discovered by suitable modification at C28 position of ursolic acid.These data suggest that ursolic acid and its derivatives represent a promising lead structural core to discover a new class of antiangiogenesis agents.