23 documents found, page 1 of 3
Extraction of Salicylic Acid Using Sustainable ATPSs and Respective Immobilizat...
Velho, P; Sousa, E; Maria Eugénia MacedoActive pharmaceutical ingredients (APIs), a class of emerging pollutants present in residual waters, are often found in hospital effluents and are known to pose profound consequences to aquatic environments, such as the feminization of fish, for which finding sustainable extractive methodologies for these chemical species is a must. Aqueous two-phase systems (ATPSs) constitute a liquid-liquid extraction techniq...
Measurement and modelling of liquid density (298.15 and 313.15 K) and vapour pr...
Velho, P; Sousa, E; Maria Eugénia MacedoDue to the eco-friendliness of organic salts, they have been gradually replacing other electrolytes in different fields of chemistry. For example, they provide biocompatible salting-out agents for liquidliquid extractions and earth-abundant materials for flow batteries. Nevertheless, reliable liquid density and vapour pressure data, which are paramount for a proper parameterisation of thermodynamic models, are ...
Sex differences in axial spondyloarthritis: data from a Portuguese spondyloarth...
Cunha, RN; Sousa, E; Khmelinskii, N; Ávila, P; Couto, M; Seixas, MI; Martins, N; Bernardes, M; Martins, A; da Silva, AB; Lourenço, MH; Miguel, CBackground: Axial spondyloarthritis (axSpA), particularly ankylosing spondylitis was historically considered a male’s disease and has been under-recognized in women. Emerging evidence reveals sex differences in pathophysiology, disease presentation and therapeutic efficacy. Objective: To identify differences between sexes in a Portuguese cohort of patients with axSpA regarding clinical manifestations, disease a...
Semi-synthesis of small molecules of aminocarbazoles: Tumor growth inhibition a...
Long, S; Loureiro, JB; Carvalho, C; Gales, L; Saraiva, L; Pinto, MMM; Puthongking, P; Sousa, EThe tumor suppressor p53 is inactivated by mutation in approximately 50% of human cancers. Small molecules that bind and stabilize those mutants may represent effective anticancer drugs. Herein, we report the tumor cell growth inhibitory activity of carbazole alkaloids and amino derivatives, as well as their potential activation of p53. Twelve aminocarbazole alkaloids were semi-synthesized from heptaphylline (1...
Tetracyclic thioxanthene derivatives: Studies on fluorescence and antitumor act...
Durães, F; Silva, PMA; Novais, P; Amorim, I; Gales, L; Esteves, CIC; Guieu, S; Bousbaa, H; Pinto, M; Sousa, EThioxanthones are bioisosteres of the naturally occurring xanthones. They have been described for multiple activities, including antitumor. As such, the synthesis of a library of thioxanthones was pursued, but unexpectedly, four tetracyclic thioxanthenes with a quinazoline– chromene scaffold were obtained. These compounds were studied for their human tumor cell growth inhibition activity, in the cell lines A375...
Determination of the absolute configuration of bioactive indole-containing pyra...
Long, S; Furlani, IL; Oliveira, JM; Resende, DISP; Silva, AMS; Gales, L; Pereira, JA; Kijjoa, A; Cass, QB; Oliveira, RV; Sousa, E; Pinto, MMMIn recent decades, fungi-derived naturally occurring quinazolines have emerged as potential drug candidates. Nevertheless, most studies are conducted for bioactivity assays, and little is known about their absorption, distribution, metabolism, and elimination (ADME) properties. To perform metabolic studies, the synthesis of the naturally occurring quinazolinone, fiscalin B (1), and its chloro derivative, 4-((1H...
Antimicrobial activity of a library of thioxanthones and their potential as eff...
Durães, F; Palmeira, A; Cruz, B; Freitas-Silva, J; Szemerédi, N; Gales, L; Costa, PM; Remião, F; Silva, R; Pinto, M; Spengler, G; Sousa, EThe overexpression of efflux pumps is one of the causes of multidrug resistance, which leads to the inefficacy of drugs. This plays a pivotal role in antimicrobial resistance, and the most notable pumps are the AcrAB-TolC system (AcrB belongs to the resistance-nodulation-division family) and the NorA, from the major facilitator superfamily. In bacteria, these structures can also favor virulence and adaptation m...
Preliminary virtual screening studies to identify grp78 inhibitors which may in...
Palmeira, A; Sousa, E; Köseler, A; Sabirli, R; Gören, T; Türkçüer, I; Kurt, Ö; Pinto, MM; Vasconcelos, MHSARS-CoV-2 Spike protein was predicted by molecular docking to bind the host cell surface GRP78, which was suggested as a putative good molecular target to inhibit Covid-19. We aimed to confirm that GRP78 gene expression was increased in blood of SARS-CoV-2 (+) versus SARS-CoV-2 (-) pneumonia patients. In addition, we aimed to identify drugs that could be repurposed to inhibit GRP78, thus with potential anti-SA...
Design and synthesis of new inhibitors of p53–MDM2 interaction with a chalcone ...
Pereira, D; Lima, RT; Palmeira, A; Seca, H; Soares, J; Gomes, S; Raimundo, L; Maciel, C; Pinto, M; Sousa, E; Vasconcelos, MH; Saraiva, L; Cidade, HThe virtual screening of a library of chalcone derivatives led us to the identification of potential new MDM2 ligands. The chalcones with the best docking scores obeying the Lipinski rule of five were subsequently prepared by base-catalyzed aldol reactions. The activity of these compounds as inhibitors of p53–MDM2 interaction was investigated using a yeast-based screening assay. Using this approach two chalcone...
Synthesis of new proteomimetic quinazolinone alkaloids and evaluation of their ...
Long, S; Resende, D; Kijjoa, A; Silva, A; Fernandes, R; Xavier, CPR; Vasconcelos, MH; Sousa, E; Pinto, MNew quinazolinone derivatives of the marine-derived alkaloids fiscalin B (3) and fumiquinazoline G (1), with neuroprotective and antitumor effects, were synthesized. Eleven quinazolinone-containing indole alkaloids were synthesized, proceeding the anti analogs via a one-pot method, and the syn analogs by the Mazurkiewicz-Ganesan approach. The neuroprotection capacity of these compounds on the rotenone-damage hu...