Unravelling the anticancer potential of functionalized chromeno[2,3-b]pyridines for breast cancer treatment
2020; Elsevier BV; Volume: 100; Linguagem: Inglês
10.1016/j.bioorg.2020.103942
ISSN1090-2120
AutoresSofia Oliveira-Pinto, Olívia Pontes, Diogo Lopes, Belém Sampaio‐Marques, Marta D. Costa, L. Carvalho, Céline S. Gonçalves, Bruno M. Costa, Patrı́cia Maciel, Paula Ludovico, Fátima Baltazar, M. Fernanda R. P. Proença, Marta Costa,
Tópico(s)Synthesis and biological activity
ResumoA 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 G2/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.
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