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Title: | C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Activities and Docking Studies | Authors: | Canário, Catarina Matias, Mariana Brito, Vanessa Pires, Patrícia Santos, Adriana O. Falcão, Amílcar Silvestre, Samuel Alves, Gilberto |
Keywords: | C-ring; cytotoxic; docking; estrogenicity; estrone | Issue Date: | 2022 | Project: | POCI-01-0145-FEDER-007491 UID/Multi/00709/2019 CENTRO-01-0145-FEDER-000013 |
Serial title, monograph or event: | Applied Sciences (Switzerland) | Volume: | 12 | Issue: | 7 | 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. | URI: | https://hdl.handle.net/10316/100517 | ISSN: | 2076-3417 | DOI: | 10.3390/app12073579 | Rights: | openAccess |
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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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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