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) an...

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Bibliographic Details
Published in:Chemistry of natural compounds 2022-09, Vol.58 (5), p.882-887
Main Authors: Li, Chunshi, Zhang, Tianyi, Zhang, Qiaosi, Liu, Xin, Zou, Jixin, Bai, Xueqian
Format: Article
Language:English
Subjects:
Biological activity
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Hypoxia
Organic Chemistry
Plant Sciences
Synthesis
Triazoles
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Summary: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.
ISSN:0009-3130
1573-8388
DOI:10.1007/s10600-022-03821-8