Anticancer Activity of Phenolic Acids of Natural or Synthetic Origin:  A Structure−Activity Study

• Autor(a) principal: Gomes, Catarina A.
• Data de Publicação: 2003
• Outros Autores: Cruz, Teresa Girão da, Andrade, José L., Milhazes, Nuno, Borges, Fernanda, Marques, M. Paula M.
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10316/45155; https://doi.org/10.1021/jm030956v
• topic: Adenocarcinoma; Antineoplastic Agents; Breast Neoplasms; Caffeic Acids; Cell Division; Cell Line, Tumor; Cell Survival; Drug Screening Assays, Antitumor; Female; Gallic Acid; Humans; Leukemia, Lymphoid; Magnetic Resonance Spectroscopy; Models, Molecular; Molecular Conformation; Phenols; Spectrometry, Mass, Electrospray Ionization; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared; Structure-Activity Relationship; Uterine Cervical Neoplasms

Several phenolic acids-caffeic and gallic acid derivatives-were synthesized and screened for their potential antiproliferative and cytotoxic properties, in different human cancer cell lines: mammary gland and cervix adenocarcinomas and lymphoblastic leukemia. The selected phenols were structurally related, which allowed us to gather important information regarding the structure-activity relationships underlying the biological activity of such compounds. This is proposed to be due to a balance between the antioxidant and pro-oxidant properties of this kind of agent. Distinct effects were found for different cell lines, which points to a significant specificity of action of the drugs tested. It was verified, for the types of cancer investigated, that the trihydroxylated derivatives yielded better results than the dihydroxylated ones. Tests in noncancerous cells, human lung fibroblasts, were also undertaken, in view of determining the toxic side effects of the compounds studied.