Affiliation:
1. Graduate Program in Chemistry Department of Chemistry Federal University of Espírito Santo, UFES Vitória 29075-910 Brazil
2. Department of Pharmacology Institute of Biomedical Sciences University of São Paulo São Paulo, SP 05508-000 Brazil
3. São Carlos Institute of Physics University of São Paulo São Carlos, SP PO Box 369, 13560–970 Brazil
Abstract
AbstractPaeonol 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a methodology previously employed by our research group, 11 derivatives of paeonol were synthesized (seven of them are unpublished compounds), including four ethers and seven benzofurans.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.
Funder
Conselho Nacional de Desenvolvimento Científico e Tecnológico
Fundação de Amparo à Pesquisa do Estado de São Paulo