Synthesis of cytotoxic benzofurans and ethers derivatives of paeonol.
FIGUEROA, Laura Patricia Rocha; DOMINGOS, Helori Vanni; PARDO, Jennifer Blandon; SANTIAGO, Pedro Henrique de Oliveira; ELLENA, Javier; LACERDA JÚNIOR, Valdemar; COSTA-LOTUFO, Letícia Veras; BORGES, Warley de Souza.
FIGUEROA, Laura Patricia Rocha; DOMINGOS, Helori Vanni; PARDO, Jennifer Blandon; SANTIAGO, Pedro Henrique de Oliveira; ELLENA, Javier; LACERDA JÚNIOR, Valdemar; COSTA-LOTUFO, Letícia Veras; BORGES, Warley de Souza.
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a methodology previously employed by our research group, 11 derivatives of paeonol were synthesized (seven of them are unpublished compounds), including four ethers and seven benzofurans.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.
@article={003218778,author = {FIGUEROA, Laura Patricia Rocha; DOMINGOS, Helori Vanni; PARDO, Jennifer Blandon; SANTIAGO, Pedro Henrique de Oliveira; ELLENA, Javier; LACERDA JÚNIOR, Valdemar; COSTA-LOTUFO, Letícia Veras; BORGES, Warley de Souza.},title={Synthesis of cytotoxic benzofurans and ethers derivatives of paeonol},journal={Chemistry and Biodiversity},note={v. 21, n. 10, p. e202400943-1-e202400943-8},year={2024}}