8 documents found, page 1 of 1
Synthesis, In Vitro Biological Evaluation of Antiproliferative and Neuroprotect...
Brito, Vanessa; Marques, Mariana; Esteves, Marta; Serra-Almeida, Catarina; Alves, Gilberto; Almeida, Paulo; Bernardino, Liliana; Silvestre, SamuelSteroids constitute an important class of pharmacologically active molecules, playing key roles in human physiology. Within this group, 16E-arylideneandrostane derivatives have been reported as potent anti-cancer agents for the treatment of leukemia, breast and prostate cancers, and brain tumors. Additionally, 5α,6α-epoxycholesterol is an oxysterol with several biological activities, including regulation of cel...
New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploi...
Guedes, Romina A.; Grilo, Jorge H.; Carvalho, Andreia N.; Fernandes, Pedro M. P.; Ressurreição, Ana S.; Brito, Vanessa; Santos, Adriana O.Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin-proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance to existing therapies and the occurrence of severe adverse effects is still a concern. The purpose of this study was the discovery of novel scaffolds of protea...
C-Ring Oxidized Estrone Acetate Derivatives: Assessment of Antiproliferative Ac...
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Pires, Patrícia; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoC-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 ...
New Estrone Oxime Derivatives: Synthesis, Cytotoxic Evaluation and Docking Studies
Canário, Catarina; Matias, Mariana; Brito, Vanessa; Santos, Adriana O.; Falcão, Amílcar; Silvestre, Samuel; Alves, GilbertoThe interest in the introduction of the oxime group in molecules aiming to improve their biological effects is increasing. This work aimed to develop new steroidal oximes of the estrane series with potential antitumor interest. For this, several oximes were synthesized by reaction of hydroxylamine with the 17-ketone of estrone derivatives. Then, their cytotoxicity was evaluated in six cell lines. An estrogenici...
Highlights on Steroidal Arylidene Derivatives as a Source of Pharmacologically ...
Brito, Vanessa; Alves, Gilberto; Almeida, Paulo; Silvestre, SamuelSteroids constitute a unique class of chemical compounds, playing an important role in physiopathological processes, and have high pharmacological interest. Additionally, steroids have been associated with a relatively low toxicity and high bioavailability. Nowadays, multiple steroidal derivatives are clinically available for the treatment of numerous diseases. Moreover, different structural modifications on th...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L. [UNESP]; Pavan, Fernando R. [UNESP]; Gomes, Clara S.B.Made available in DSpace on 2021-06-25T11:09:35Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-03-01; Schiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1–4), are synthesized. All compounds are characterized by elemental analyses, inf...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Ramilo-Gomes, Filipa; Alemu, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L.; Pavan, Fernando R.; Gomes, Clara S.B.; Brito, VanessaSchiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn2(...
Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zi...
Gomes, Filipa Ramilo; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Campos, Débora L.; Pavan, Fernando R.; Gomes, Clara S.B.; Brito, VanessaSchiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), o-vanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)-complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn2(...