Synthesis of Cytotoxic Benzofurans and Ethers Derivatives of Paeonol

Autor(es)

Figueroa, Laura P. R. ; Domingos, Helori V. ; Pardo, Jennifer B. ; Santiago, Pedro H. O. ; Ellena, Javier ; Lacerda, Valdemar ; Costa-Lotufo, Leticia V. ; Borges, Warley de S.

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 21, n. 10, p. 8-pg., 2024-10-01.

Resumo

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a methodology previously employed by our research group, 11 derivatives of paeonol were synthesized (seven of them are unpublished compounds), including four ethers and seven benzofurans.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 mu M and was selected for further analysis, results reinforce its anticancer potential. (AU)

• Processo FAPESP: 15/17177-6 - Abordagem integrada na prospecção sustentável de produtos naturais marinhos: da diversidade a substâncias anticâncer
• Beneficiário: Leticia Veras Costa Lotufo
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Temático
• Processo FAPESP: 14/50926-0 - INCT 2014: biodiversidade e produtos naturais
• Beneficiário: Vanderlan da Silva Bolzani
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Temático
• Processo FAPESP: 21/10066-5 - Estudo cristalográfico e estrutural de novas substâncias com potenciais atividades biológicas
• Beneficiário: Pedro Henrique de Oliveira Santiago
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado