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https://hdl.handle.net/1822/72841
Título: | Unravelling the anticancer potential of functionalized chromeno[2,3-b ] pyridines for breast cancer treatment |
Autor(es): | Oliveira-Pinto, Sofia Pontes, Olivia Lopes, Diogo Marques, Maria Belém Sousa Sampaio Costa, Marta D. Carvalho, Luisa Goncalves, Celine S. Costa, Bruno Marques Maciel, P. Ludovico, Paula Baltazar, Fátima Proença, M. Fernanda R. P. Costa, Marta |
Palavras-chave: | Anticancer activity Breast cancer C. elegans Chromeno[2,3-b]pyridine |
Data: | 2020 |
Editora: | Academic Press |
Revista: | Bioorganic Chemistry |
Citação: | Oliveira-Pinto, S., Pontes, O., Lopes, D., Sampaio-Marques, B., Costa, M. D., Carvalho, L., . . . Costa, M. (2020). Unravelling the anticancer potential of functionalized chromeno[2,3-b]pyridines for breast cancer treatment. Bioorganic Chemistry, 100, 103942. doi: https://doi.org/10.1016/j.bioorg.2020.103942 |
Resumo(s): | A selection of new chromeno[2,3-b]pyridines was prepared from chromenylacrylonitriles and N-substituted piperazines, using a novel and efficient synthetic procedure. The compounds were tested for their anticancer activity using breast cancer cell lines MCF-7, Hs578t and MDA-MB-231 and the non-neoplastic cell line MCF-10A for toxicity evaluation. In general, compounds showed higher activity towards the luminal breast cancer subtype (MCF-7), competitive with the reference compound Doxorubicin. The in vivo toxicity assay using C. elegans demonstrated a safe profile for the most active compounds. Chromene 3f revealed a promising drug profile, inhibiting cell growth and proliferation, inducing cell cycle arrest in G /M phase, apoptosis and microtubule destabilization. The new compounds presented exciting bioactive features and may be used as lead compounds in cancer related drug discovery. 2 |
Tipo: | Artigo |
URI: | https://hdl.handle.net/1822/72841 |
DOI: | 10.1016/j.bioorg.2020.103942 |
ISSN: | 0045-2068 |
Versão da editora: | https://linkinghub.elsevier.com/retrieve/pii/S0045206820308920 |
Arbitragem científica: | yes |
Acesso: | Acesso restrito UMinho |
Aparece nas coleções: | CDQuim - Artigos (Papers) |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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1-s2.0-S0045206820308920-main.pdf Acesso restrito! | 3,75 MB | Adobe PDF | Ver/Abrir |