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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 
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.
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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