Screening of Ursolic Acid Analogs with HIF-1α and COX-2-Inhibiting Effects

Three novel series of derivatives by introducing a 1,2,3-triazoles moiety, 1,2,4-triazoles moiety or a nitroimidazoles ring to the ursolic acid (UA) nucleus were designed and synthesized. The biological activity of these compounds was evaluated to assess their hypoxia-inducible factor-1α (HIF-1α) and cyclooxygenase-2 (COX-2) inhibitory activities along with HIF-1α inhibitory and anti-inflammatory effects. Compound 7e exhibited the highest activity of all the synthesized compounds, which was higher activity than observed for the positive control UA.