Utilize este identificador para referenciar este registo: https://hdl.handle.net/1822/80578

TítuloDiscovery of the anticancer activity for lung and gastric cancer of a brominated coelenteramine analog
Autor(es)González-Berdullas, Patricia
Pereira, Renato B.
Teixeira, Cláudia
Silva, José Pedro
Magalhães, Carla M.
Rodríguez-Borges, José E.
Pereira, David M.
Silva, Joaquim C. G. Esteves da
Silva, Luís Pinto da
Data27-Jul-2022
EditoraMultidisciplinary Digital Publishing Institute
RevistaInternational Journal of Molecular Sciences
CitaçãoGonzález-Berdullas, P.; Pereira, R.B.; Teixeira, C.; Silva, J.P.; Magalhães, C.M.; Rodríguez-Borges, J.E.; Pereira, D.M.; Esteves da Silva, J.C.G.; Pinto da Silva, L. Discovery of the Anticancer Activity for Lung and Gastric Cancer of a Brominated Coelenteramine Analog. Int. J. Mol. Sci. 2022, 23, 8271. https://doi.org/10.3390/ijms23158271
Resumo(s)Cancer is still a challenging disease to treat, both in terms of harmful side effects and therapeutic efficiency of the available treatments. Herein, to develop new therapeutic molecules, we have investigated the anticancer activity of halogenated derivatives of different components of the bioluminescent system of marine Coelenterazine: Coelenterazine (<b>Clz</b>) itself, Coelenteramide (<b>Clmd</b>), and Coelenteramine (<b>Clm</b>). We have found that <b>Clz</b> derivatives possess variable anticancer activity toward gastric and lung cancer. Interestingly, we also found that both brominated <b>Clmd</b> (<b>Br-Clmd</b>) and <b>Clm</b> (<b>Br-Clm</b>) were the most potent anticancer compounds toward these cell lines, with this being the first report of the anticancer potential of these types of molecules. Interestingly, <b>Br-Clm</b> possessed some safety profile towards noncancer cells. Further evaluation revealed that the latter compound induced cell death via apoptosis, with evidence for crosstalk between intrinsic and extrinsic pathways. Finally, a thorough exploration of the chemical space of the studied <b>Br-Clm</b> helped identify the structural features responsible for its observed anticancer activity. In conclusion, a new type of compounds with anticancer activity toward gastric and lung cancer was reported and characterized, which showed interesting properties to be considered as a starting point for future optimizations towards obtaining suitable chemotherapeutic agents.
TipoArtigo
DescriçãoSupplementary Materials: The following supporting information can be downloaded at: https: //www.mdpi.com/article/10.3390/ijms23158271/s1.
URIhttps://hdl.handle.net/1822/80578
e-ISSN1422-0067
Arbitragem científicayes
AcessoAcesso aberto
Aparece nas coleções:BUM - MDPI

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