Functionalization of gold nanoparticles with two aminoalcohol-based quinoxaline derivatives for targeting phosphoinositide 3-kinases (PI3Kα)

Silva, Janine de Araújo; Menezes, Fabrício Gava; Athayde, Heloiza Fernanda Oliveira da Silva; Vieira, Davi Serradella; Silva, Sérgio Ruschi Bergamachi; Bortoluzzi, Adailton J.; Sant’Anna, Celso; Eugenio, Mateus; Neri, Jannyely Moreira; Gasparotto, Luiz Henrique da Silva

Functionalization of gold nanoparticles with two aminoalcohol-based quinoxaline derivatives for targeting phosphoinositide 3-kinases (PI3Kα)

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dc.contributor.author	Silva, Janine de Araújo
dc.contributor.author	Menezes, Fabrício Gava
dc.contributor.author	Athayde, Heloiza Fernanda Oliveira da Silva
dc.contributor.author	Vieira, Davi Serradella
dc.contributor.author	Silva, Sérgio Ruschi Bergamachi
dc.contributor.author	Bortoluzzi, Adailton J.
dc.contributor.author	Sant’Anna, Celso
dc.contributor.author	Eugenio, Mateus
dc.contributor.author	Neri, Jannyely Moreira
dc.contributor.author	Gasparotto, Luiz Henrique da Silva
dc.date.accessioned	2020-08-06T14:55:23Z
dc.date.available	2020-08-06T14:55:23Z
dc.date.issued	2018-12-17
dc.description.resumo	Quinoxaline derivatives have attracted considerable attention due to their vast range of applications that includes electroluminescence and biomedicine. Concerning the latter, the literature has shown that compounds with a quinoxaline motif bind quite efficiently to phosphatidylinositol-4,5-bisphosphate 3-kinases (PI3Ks), which are enzymes found to be overexpressed in some types of neoplasms. In the present study, gold nanoparticles (AuNPs) were easily functionalized with 2,3-diethanolminoquinoxaline (DEQX) and 2-(2,3-dihydro-[1,4]oxazino[2,3-b]quinoxalin-4-yl)ethanol (OAQX). We made use of glycerol in alkaline media as reducing agent and the quinoxalines served as capping ligands to stabilize the AuNPs. This is the first report on the modification of a nanostructure with quinoxalines. Functionalization confers nanoparticles the required specificity to target only cancer cells, which opens possibilities for phototherapy since the modified AuNPs would concentrate in the tumor tissue as a consequence of PI3Kα overexpression. Molecular dynamics simulations have shown that DEQX and OAQX are potential inhibitors of PI3Kα since they bind to the active site of the enzyme in a way similar to other known inhibitors.	pt_BR
dc.identifier.citation	ARAÚJO, Janine; MENEZES, Fabrício G.; SILVA, Heloiza F. O.; VIEIRA, Davi S.; SILVA, Sergio R. B.; BORTOLUZZI, Adailton J.; SANT’ANNA, Celso; EUGENIO, Mateus; NERI, Jannyely M.; GASPAROTTO, Luiz H. S. Functionalization of gold nanoparticles with two aminoalcohol-based quinoxaline derivatives for targeting phosphoinositide 3-kinases (PI3Kα). New Journal Of Chemistry, [S.l.], v. 43, n. 4, p. 1803-1811, 2019. http://dx.doi.org/10.1039/c8nj04314k. Disponível em: https://pubs.rsc.org/en/content/articlelanding/2019/nj/c8nj04314k#!divAbstract. Acesso em: 6 ago. 2020.	pt_BR
dc.identifier.doi	10.1039/C8NJ04314K
dc.identifier.uri	https://repositorio.ufrn.br/jspui/handle/123456789/29787
dc.language	en	pt_BR
dc.publisher	Royal Society of Chemistry (RSC)	pt_BR
dc.subject	Quinoxalines	pt_BR
dc.subject	Phosphoinositide-3 kinase inhibitors	pt_BR
dc.title	Functionalization of gold nanoparticles with two aminoalcohol-based quinoxaline derivatives for targeting phosphoinositide 3-kinases (PI3Kα)	pt_BR
dc.type	article	pt_BR