Accessing Promising Passerini Adducts in Anticancer Drug Design.

The 3-component Passerini reaction (3CPR), discovered little more than 100 years ago, has been demonstrated in the last few decades to be a valuable tool for accessing structural diversity and complexity, essential topics to consider in drug discovery programs. Focusing on accessing a fine-tuned family of α-acyloxyamide-oxindole hybrids, we underline herein our latest insights regarding the use of this mild reaction approach to obtain promising anticancer agents. Cheap and commercially available isatin was used as starting material.

Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insights on Synthetic Strategies.

Vascular endothelial growth factor receptor 2 (VEGFR-2) is a crucial mediator of angiogenesis, playing a pivotal role in both normal physiological processes and cancer progression. Tumors harness VEGFR-2 signaling to promote abnormal blood vessel growth, which is a key step in the metastasis process, making it a valuable target for anticancer drug development. While there are VEGFR-2 inhibitors approved for therapeutic use, they face challenges like drug resistance, off-target effects, and adverse side effects, limiting their effectiveness.

Affordable Small Molecules as Promising Fluorescent Labels for Biomolecules.

Fluorescent labels, commonly used in highly sensitive analytical techniques for detecting and tracking biomolecules in critical fields like cellular biology, medicine, medicinal chemistry, and environmental science, are currently too expensive for routine use in standard applications, with most exhibiting small Stokes shifts. This limitation underscores the potential of 4-diethylaminobenzaldehyde derivatives as a cost-effective alternative for developing new, bright fluorophores with larger Stokes shifts. In this work, using 4-diethylaminobenzaldehyde as starting material, we developed a simple, cost-effective, and efficient synthetic strategy to produce new affordable small molecules as effective fluorescent labels for biomolecules.

Effects of body-oriented intervention after stroke on cognitive function, body awareness, and quality of life: A systematic review.

Background: Some cognitive functions can be affected by a stroke as it causes sensory, perceptual, and visual deficits, contributing to a loss of body awareness and changes in one's body image and leading to a decrease in the quality of life (QoL). This systematic review aims to identify and systematize scientific evidence of body-oriented intervention (BOI) effects in adult and elderly patients after a stroke on cognitive function, body awareness, and QoL.

Methods: The research was carried out in: Pubmed, Science Direct, Cochrane, Web of Science, Psycinfo, Scopus, Portal Regional da BVS, and PEDro.

Airborne DNA: State of the art - Established methods and missing pieces in the molecular genetic detection of airborne microorganisms, viruses and plant particles.

Bioaerosol is composed of different particles, originating from organisms, or their fragments with different origin, shape, and size. Sampling, analysing, identification and describing this airborne diversity has been carried out for over 100 years, and more recently the use of molecular genetic tools has been implemented. However, up to now there are no established protocols or standards for detecting airborne diversity of bacteria, fungi, viruses, pollen, and plant particles.

Assessing the Potential of 1,2,3-Triazole-Dihydropyrimidinone Hybrids Against Cholinesterases: In Silico, In Vitro, and In Vivo Studies.

Combining the pharmacological properties of the 1,2,3-triazole and dihydropyrimidinone classes of compounds, two small families of mono- and di(1,2,3-triazole)-dihydropyrimidinone hybrids, A and B, were previously synthesized. The main objective of this work was to investigate the potential anti-Alzheimer effects of these hybrids. The inhibitory activities of cholinesterases (AChE and BuChE), antioxidant activity, and the inhibitory mechanism through in silico (molecular docking) and in solution (STD-NMR) experiments were evaluated.

Evaluating building stones: Physical-mechanical changes from high-temperature fire and water cooling.

Heritage sites built with natural stone are at risk from fires, which can alter stone properties and compromise its structural integrity. Over 60 studies in the past three decades have examined fire impact on natural stone, providing insights for their prevention and restoration. The primary objectives are to develop effective strategies to mitigate fire risks, protect heritage structures, and ensure the preservation of our cultural legacy.

Protein Hydrolysates from Salmon Heads and Cape Hake By-Products: Comparing Enzymatic Method with Subcritical Water Extraction on Bioactivity Properties.

Fish by-products can be converted into high-value-added products like fish protein hydrolysates (FPHs), which have high nutritional value and are rich in bioactive peptides with health benefits. This study aims to characterise FPHs derived from salmon heads (HPSs) and Cape hake trimmings (HPHs) using Alcalase for enzymatic hydrolysis and Subcritical Water Hydrolysis (SWH) as an alternative method. All hydrolysates demonstrated high protein content (70.

Numerical Analysis of the Porous Structure of Activated Carbons Derived from Synthetic Polymers.

This paper presents original results from the unique analysis of the porous structure of activated carbons (ACs) produced through the chemical activation of polyethylene terephthalate (PET) and polyacrylonitrile (PAN), as well as from a physical mixture of both polymers. An advanced method of adsorbent surface analysis-more specifically, the new method of numerical clustering-based adsorption analysis regarding the surface heterogeneity, pore geometry and adsorption energy distribution parameters-allowed us to obtain information about the porous structure of the ACs from the synthetic polymers mentioned above. As the results showed, ACs obtained with PAN were characterised by a first adsorbed layer with the highest volume.

The Ugi4CR as effective tool to access promising anticancer isatin-based α-acetamide carboxamide oxindole hybrids.

Considering early-stage drug discovery programs, the Ugi four-component reaction is a valuable, flexible, and pivotal tool, facilitating the creation of two new amide bonds in a one-pot fashion to effectively yield the desired α-aminoacylamides. Here, we highlight the reputation of this reaction approach to access number and scaffold diversity of a library of isatin-based α-acetamide carboxamide oxindole hybrids, promising anticancer agents, in a mild and fast sustainable reaction process. The library was tested against six human solid tumor cell lines, among them, non-small cell lung carcinoma, cervical adenocarcinoma, breast cancer and colon adenocarcinoma.

Mackerel and Seaweed Burger as a Functional Product for Brain and Cognitive Aging Prevention.

Most world countries are experiencing a remarkable aging process. Meanwhile, 50 million people are affected by Alzheimer's disease (AD) and related dementia and there is an increasing trend in the incidence of these major health problems. In order to address these, the increasing evidence suggesting the protective effect of dietary interventions against cognitive decline during aging may suggest a response to this challenge.

Asymmetric Additions Empowered by OrganoCatalysts, Metal Catalysts, and Deep Natural Eutectic Solvents (NADES).

This article is a history of an industrial-academic partnership that started almost two decades ago and details the evolution of a relationship between a small academic research group and a spin-out company located in Portugal. Their activities have ranged from the development of new metal-based catalytic systems for asymmetric epoxidations, allylic alkylations, and arylations to the development of novel cinchona-based organocatalysts for asymmetric hydrosilylations and Michael additions. Current common interests are centered on the development of novel chiral Natural Deep Eutectic Solvent systems, which they are investigating in different types of reaction systems.

New Forms of Neuroactive Phospholipids for DHA Enrichment in Brain.

Low levels of docosahexaenoic acid (DHA) in the brain have been related to neurological disorders, like Alzheimer's disease (AD). After ingestion, dietary DHA must cross the blood-brain barrier, where it is absorbed as lysophosphatidylcholine (LPC), due to its role as a preferential DHA carrier in the brain. This work aimed at the production of LPC-DHA extracts to be used in supplementation/food fortification intended neural enrichment in DHA.

Influence of cooking methods and storage time on colour, texture, and fatty acid profile of a novel fish burger for the prevention of cognitive decline.

Western diets are poor in healthy n-3 polyunsaturated fatty acids (n-3 PUFA), namely eicosapentaenoic (EPA) and docosahexaenoic acid (DHA), iodine (I), and other nutrients that may protect against cognitive ageing. Given DHA richness in chub mackerel (), high vitamin B9 levels in quinoa (), and I abundance in the seaweed , a functional hamburger rich in these nutrients by using these ingredients was developed. This research focused on the factors affecting its quality by examining the impact of cooking (steaming at 100 °C, roasting at 180 °C, grilling at 180 °C) and storage time (after 4 and 6 months at -20 °C) upon the product's properties.

Ecotoxicological responses of juvenile Sparus aurata to BDE-99 and BPA exposure: A multi-biomarker approach integrating immune, endocrine and oxidative endpoints.

Pentabromodiphenyl ether (BDE-99) and bisphenol A (BPA) are synthetic organic compounds present in several daily use products. Due to their physicochemical properties, they are ubiquitously present in aquatic ecosystems and considered highly persistent. Recent evidence has confirmed that both emerging compounds are toxic to humans and terrestrial mammals eliciting a wide range of detrimental effects at endocrine and immune levels.

Metal-catalyzed coupling/carbonylative cyclizations for accessing dibenzodiazepinones: an expedient route to clozapine and other drugs.

A sequential strategy to access 10,11-dihydro-5-dibenzo[,][1,4]diazepinones (DBDAPs) is disclosed in this article through a palladium and copper-catalyzed amination (Buchwald-Hartwig (B-H) or Chan-Lam (C-L)) followed by a palladium-catalyzed intramolecular aminocarbonylation with Mo(CO) as CO surrogate (to avoid toxic CO handling) of readily available -phenylenediamines and either 1,2-dibromobenzene or 2-bromophenylboronic acid. The 10,11-dihydro-5-dibenzo[,][1,4]diazepinone could be synthezised in good yield using a sequential catalytic procedure, using both C-L and B-H approaches. Gratifingly, the use of the C-L reaction was more impressive, and afforded the dibenzodiazepinones in good yields (up to 45%; 2 steps) and much milder conditions using copper as the catalyst.

Exploring Omega-3's Impact on the Expression of Bone-Related Genes in Meagre ().

Dietary supplementation with Omega-3 fatty acids seems to promote skeletal health. Therefore, their consumption at imbalanced or excessive levels has offered less beneficial or even prejudicial effects. Fish produced in aquaculture regimes are prone to develop abnormal skeletons.

Dataset of the complete mitogenome of the deep-sea sailfin roughshark, Frade, 1929.

Chondrichthyans comprise a diverse group of vertebrate species with extraordinary ecological relevance. Yet, multiple members of this evolutionary lineage are associated with significant extinction risk. The sailfin roughshark is a deep-water benthic shark currently listed as vulnerable due to population declines in parts of its range.

Quercetin-1,2,3-Triazole Hybrids as Multifunctional Anti-Alzheimer's Agents.

The number of patients with Alzheimer's disease (AD) continues to rise and, despite the efforts of researchers, there are still no effective treatments for this multifaceted disease. The main objective of this work was the search for multifunctional and more effective anti-Alzheimer agents. Herein, we report the evaluation of a library of quercetin-1,2,3-triazole hybrids () in antioxidant, hydrogen peroxide-induced oxidative stress protection, and cholinesterases (AChE and BuChE) inhibitory activities.

Microplastics in marine mussels, biological effects and human risk of intake: A case study in a multi-stressor environment.

This study documented seasonal levels of microplastics (MPs) and biomarkers (condition index, neurotoxicity, energy, oxidative stress) in mussels (Mytilus galloprovincialis), and water physico-chemical parameters in the Douro estuary (NE Atlantic coast), and estimated the human risk of MP intake (HRI) through mussels. Mussel stress was determined through the Integrated Biomarker Response (IBR). HRI was estimated from mussel MP concentrations and consumer habits.

Rational Design of Cost-Effective 4-Styrylcoumarin Fluorescent Derivatives for Biomolecule Labeling.

Fluorescent labels are key tools in a wide range of modern scientific applications, such as fluorescence microscopy, flow cytometry, histochemistry, direct and indirect immunochemistry, and fluorescence in situ hybridization (FISH). Small fluorescent labels have important practical advantages as they allow maximizing the fluorescence signal by binding multiple fluorophores to a single biomolecule. At present, the most widely used fluorescent labels available present small Stokes shifts and are too costly to be used in routine applications.