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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ACKNOWLEDGMENT
This work was supported by the Natural Science Foundation of Jilin Province (No. 20210101420JC); the Department of Education of Jilin Province (No. JJKH20210495KJ); and the Health Department of Jilin Province (2020Z005). The authors Chunshi Li and Tianyi Zhang contributed equally to this work.
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Published in Khimiya Prirodnykh Soedinenii, No. 5, September–October, 2022, pp. 743–747.
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Li, C., Zhang, T., Zhang, Q. et al. Screening of Ursolic Acid Analogs with HIF-1α and COX-2-Inhibiting Effects. Chem Nat Compd 58, 882–887 (2022). https://doi.org/10.1007/s10600-022-03821-8
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DOI: https://doi.org/10.1007/s10600-022-03821-8