Alexandra M. M. Antunes

Ni(II) Complexes of 2-Imine-8-Hydroxyquinolines: Characterization, Albumin Binding and Cytotoxicity

Sofia Marcão, Leonor Côrte‐Real, Alice Alborghetti, Maël Dejoux et autres

Nickel(II) offers an appealing base for metallodrug design as it is abundant, inexpensive and forms well-defined complexes with N,O-donor ligands. Therefore, five Ni(II) complexes containing two tridentate 2-imine-8-hydroxyquinoline Schiff base ligands, derived from morpholine, piperidine, imidazole or 2-methyl-1H-limidazole, were synthesized and characterized …

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Covalent Targeting and Thermostabilization of Oncogenic R280K and R273H Mutants p53 by Small Molecule RVJB59

Ricardo J. F. Ferreira, Lídia Gonçalves, Mattia Mori, Alexandra M. M. Antunes et autres

Breast cancer is one of the most common cancers worldwide. Approximately 30%-40% of breast cancers harbor mutations in the TP53 gene, leading to structural and functional alterations in the p53 protein. These changes result in mutant proteins that are unable to perform …

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s-cysteinylation of proteins is modulated by human cystathionine β-synthase and cystathionine γ-lyase

Dalila Fernandes, António B. Pimpão, Antonio Melo Junior, Catarina Tomé et autres

N-desethyl isotonitazene in fake oxycodone tablets seized in Portugal: the first notification in Europe

Carla Ferreira, Alexandra M. M. Antunes, Helena Gaspar, Maria João Caldeira

Nitazenes class emerged in the mid-1950s as an attempt to develop safer and more effective opioid analgesics for medical applications. This led to the discovery of a series of 2-benzylbenzimidazole derivatives, which exhibited analgesic potency several orders of magnitude higher than that …

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The cytotoxicity of synthetic cathinones on dopaminergic-differentiated SH-SY5Y neuroblastoma cell line: Exploring the role of β-keto metabolic reduction

Rita P. Lopes, Cláudia C. Miranda, Tiago G. Fernandes, Helena Gaspar et autres

Synthetic cathinones, a major class of new psychoactive substances (NPS), pose a growing public health threat due to their widespread recreational use, particularly among young people. While metabolism significantly influences xenobiotic toxicity, its role in synthetic cathinone neurotoxicity remains underexplored. Similarly to …

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Mechanistic Insights of a p53-Targeting Small Molecule

Ricardo J. Ferreira, Valentina Barcherini, Catarina Roma‐Rodrigues, Miriama Sikorová et autres

High Resolution Image Download MS PowerPoint Slide Restoring the p53 pathway, particularly by reactivating wild-type (wt) or mutant (mut) p53, is considered a promising approach for cancer treatment. Previously, we identified the tryptophanol-derived oxazoloisoindolinone family as a new scaffold for obtaining wt …

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Novel 8-Hydroxyquinoline-Derived V(IV)O, Ni(II), and Fe(III) Complexes: Synthesis, Characterization, and In Vitro Cytotoxicity Against Tumor Cells

Joana Lopes, Leonor Côrte‐Real, Íris Neto, Alice Alborghetti et autres

We report the synthesis and characterization of five novel metal complexes. Three of them are vanadium complexes with the general formula [VO(Ln)2], where Ln are Schiff bases derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with either 4-(2-aminoethyl)morpholine (L1), 3-morpholinopropylamine (L2) or 1-(2-aminoethyl)piperidine (L3). …

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Biotransformation of ketamine in terminal in vivo experiments under chronic intermittent hypoxia conditions and the role of AhR

António B. Pimpão, Luísa Teixeira-Santos, Nuno R. Coelho, Maria João Correia et autres

We were pioneers in describing aryl hydrocarbon receptor (AhR) activation by chronic intermittent hypoxia (CIH) in a rat pre-clinical model. This model mimics hypertension (HTN) secondary to obstructive sleep apnea, enabling longitudinal investigation of hypertension development. Concerns about the influence of barbiturates …

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Monoterpenoid selenophenes derived from (−)-carvone with GPx-like activity

João P. Telo, Luı́s F. Veiros, Vânia André, João Ferreira da Silva et autres

Organoselenium compounds have been recognized as potential therapeutic agents against several diseases. Specifically, the incorporation of selenium into natural products has been reported to produce positive synergistic biological effects. We report herein the one-pot reaction of the natural monoterpenoid (-)-carvone with selenium …

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Carcinogenicity of hydrochlorothiazide, voriconazole, and tacrolimus

Vincent James Cogliano, Emanuela Corsini, Agnès Fournier, Heather H. Nelson et autres

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Regulation of mitochondrial hydrogen sulfide metabolism by endogenous modulators of persulfide dioxygenase

João B. Vicente, Diogo H.P. Silva, Francesca Giordano, D. Fernandes et autres

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The power of antibiotic coordination frameworks towards enhanced antimicrobial activity

Vânia André, Paula C. Alves, Alexandra M. M. Antunes, D. Q. Baptista et autres

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