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Updated: Jun 21, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis of Cytotoxic Benzofurans and Ethers Derivatives of Paeonol
Laura P R Figueroa1, Helori V Domingos2, Jennifer B Pardo1
1Graduate Program in Chemistry, Department of Chemistry, Federal University of Espírito Santo, UFES, Vitória, 29075-910, Brazil.
Abstract:
Paeonol is a broadly studied natural product due to its many biological activities. Using a methodology previously employed by our research group, 11 derivatives of paeonol were synthesized (seven of them are unpublished compounds), including four ethers and seven benzofurans. Additionally, we determined the crystal structure of one of these ether derivatives (1 a) and of five benzofuran derivatives (2 a, 2 b, 2 c, 2 f and 2 g) by single crystal X-ray diffraction. To continue studying the cytotoxicity of this natural product and its derivatives, all compounds were tested against two cancer cell lines, HCT116 and MCF-7. Compounds 2 b, 2 e, and 2 g were considered active against the colorectal adenocarcinoma cells HCT116 (Growth inhibition >60 %). Compound 2 e showed an IC50 of 0.2 μM and was selected for further analysis, results reinforce its anticancer potential.
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