Screening of Ursolic Acid Analogs with HIF-1α and COX-2-Inhibiting Effects
2022
Li, Chunshi | Zhang, Tianyi | Zhang, Qiaosi | Liu, Xin | Zou, Jixin | Bai, Xueqian
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.
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