Please use this identifier to cite or link to this item:
https://hdl.handle.net/10316/100517
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Canário, Catarina | - |
dc.contributor.author | Matias, Mariana | - |
dc.contributor.author | Brito, Vanessa | - |
dc.contributor.author | Pires, Patrícia | - |
dc.contributor.author | Santos, Adriana O. | - |
dc.contributor.author | Falcão, Amílcar | - |
dc.contributor.author | Silvestre, Samuel | - |
dc.contributor.author | Alves, Gilberto | - |
dc.date.accessioned | 2022-06-28T09:18:57Z | - |
dc.date.available | 2022-06-28T09:18:57Z | - |
dc.date.issued | 2022 | - |
dc.identifier.issn | 2076-3417 | pt |
dc.identifier.uri | https://hdl.handle.net/10316/100517 | - |
dc.description.abstract | C-Ring oxidized estrone acetate derivatives as antiproliferative agents were prepared and tested against five cancer cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Flow cytometry assays to evaluate cell viability and modifications in cell cycle phases and molecular docking research against estrogen receptor α, steroid sulfatase, and 17β-hydroxysteroid dehydrogenase type 1 were performed. 9α-Hydroxy,11β-nitrooxyestrone acetate was the most cytotoxic molecule against hormone-dependent cancer cells. Furthermore, flow cytometry experiments revealed that this 9α-hydroxy,11β-nitrooxy derivative markedly reduced HepaRG cells viability (~92%) after 24 h of treatment. However, 9α-hydroxyestrone acetate led to selective inhibition of HepaRG cells growth, inducing a G0/G1 cycle arrest, and did not originate a proliferation effect on T47-D cancer cells. Docking studies estimated a generally lower affinity of these compounds to estrogen receptor α than predicted for estrone and 17β-estradiol. Therefore, this structural modification can be of interest to develop new anticancer estrane derivatives devoid of estrogenic action. © 2022 by the authors. | pt |
dc.language.iso | eng | pt |
dc.relation | POCI-01-0145-FEDER-007491 | pt |
dc.relation | CENTRO-01-0145-FEDER-000013 | pt |
dc.relation | info:eu-repo/grantAgreement/FCT/UID/Multi/00709/2013 | pt |
dc.rights | openAccess | pt |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/ | pt |
dc.subject | C-ring | pt |
dc.subject | cytotoxic | pt |
dc.subject | docking | pt |
dc.subject | estrogenicity | pt |
dc.subject | estrone | pt |
dc.title | C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Activities and Docking Studies | pt |
dc.type | article | - |
degois.publication.firstPage | 3579 | pt |
degois.publication.issue | 7 | pt |
degois.publication.title | Applied Sciences (Switzerland) | pt |
dc.peerreviewed | yes | pt |
dc.identifier.doi | 10.3390/app12073579 | pt |
degois.publication.volume | 12 | pt |
dc.date.embargo | 2022-01-01 | * |
uc.date.periodoEmbargo | 0 | pt |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | open | - |
item.openairetype | article | - |
item.languageiso639-1 | en | - |
item.fulltext | Com Texto completo | - |
item.cerifentitytype | Publications | - |
crisitem.project.grantno | Health Sciences Research Centre | - |
crisitem.author.researchunit | CNC - Center for Neuroscience and Cell Biology | - |
crisitem.author.researchunit | CNC - Center for Neuroscience and Cell Biology | - |
crisitem.author.orcid | 0000-0002-3854-6549 | - |
crisitem.author.orcid | 0000-0003-4297-5108 | - |
Appears in Collections: | I&D CIBIT - Artigos em Revistas Internacionais I&D CNC - Artigos em Revistas Internacionais FFUC- Artigos em Revistas Internacionais |
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File | Description | Size | Format | |
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CRing-Oxidized-Estrone-Acetate-Derivatives-Assessment-of-Antiproliferative-Activities-and-Docking-StudiesApplied-Sciences-Switzerland.pdf | 3.49 MB | Adobe PDF | View/Open |
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