A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM IC50 values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity (IC50 > 50 μmol/L).
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Published in Khimiya Prirodnykh Soedinenii, No. 6, November–December, 2022, pp. 905–908.
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Ren, X., Cui, L., Wang, Y. et al. Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors. Chem Nat Compd 58, 1075–1078 (2022). https://doi.org/10.1007/s10600-022-03870-z
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DOI: https://doi.org/10.1007/s10600-022-03870-z