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https://hdl.handle.net/1822/58102
Título: | Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment |
Autor(es): | Pontes, Olívia Costa, Marta Sílvia Freitas Santos, Filipa Marques, Maria Belém Sousa Sampaio Dias, Tatiana Alexandra Freitas Perdigão Ludovico, Paula Baltazar, Fátima Proença, M. Fernanda R. P. |
Palavras-chave: | Antineoplastic Agents Benzopyrans Cell Proliferation Cell Survival Cells, Cultured Chalcones Dose-Response Relationship, Drug Humans Molecular Structure Structure-Activity Relationship 4H-chromenes Anticancer activity Breast cancer Michael addition |
Data: | 5-Set-2018 |
Editora: | Elsevier Masson |
Revista: | European Journal of Medicinal Chemistry |
Resumo(s): | Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure compounds. These compounds were tested on breast cancer cells (MCF-7 and Hs578T) and breast non-neoplastic cells (MCF-10A). After determination of IC50 value, specific assays were performed to analyze the potential of these compounds, and those bearing halogenated substituents presented enhanced activity comparing to methoxyl or methyl groups. More specifically, the bromine atom was often present in the bioactive molecules that proceeded to the final assays and showed to be promising candidates for further studies. The selected chromene acted as a cell migration inhibitory agent and triggered regulated cell death associated with G2/M cell-arrest and microtubule destabilization. For chalcones, the results suggest an anti-proliferative activity. Also, results for combination-therapy potentiated the antitumor effect of doxorubicin and reduced cytotoxicity in MCF-10A cells. |
Tipo: | Artigo |
URI: | https://hdl.handle.net/1822/58102 |
DOI: | 10.1016/j.ejmech.2018.07.058 |
ISSN: | 0223-5234 |
Arbitragem científica: | yes |
Acesso: | Acesso restrito UMinho |
Aparece nas coleções: | ICVS - Artigos em revistas internacionais / Papers in international journals |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment..pdf Acesso restrito! | 2,64 MB | Adobe PDF | Ver/Abrir |