A novel copper(II) complex with a salicylidene carbohydrazide ligand that promotes oxidative stress and apoptosis in triple negative breast cancer cells.

We report the synthesis, characterization, anti-cancer activity and mechanism of action of a novel water-soluble Cu(II) complex with salicylidene carbohydrazide as the ligand and -phenanthroline as the co-ligand. The synthesized complex (1) was characterized by FT-IR, EPR, and electronic spectroscopy, as well as single crystal X-ray diffraction. This compound was found to be paramagnetic from EPR spectra and X-ray crystallography revealed that the molecule crystallized in an orthorhombic crystal system.

Pd-Catalyzed Synthesis of 1-(Hetero)aryl Thioglycosides: Strategy for the Trapping of an Acyl Group of Glycosylthioesters by Coupling of Bis-Electrophilic-Nucleophilic Partners.

Herein, we describe a stereoretentive palladium-catalyzed cross-coupling between the in situ-generated glycosyl thiolate anion and diverse (hetero)aryl iodides at room temperature for creating the library of (hetero)aryl thioglycosides. The key to success is the judicious pairing of bis-electrophilic-nucleophilic partners with a variety of thioesters in an atom-economical way in which both the glycosyl thiolate anion and the acylium cation are incorporated into the final analogue. The advantage of this method is the acyl transfer on various nucleophilic partners, including a hydroxyl, a primary or secondary amine, an amino acid, and the biologically active hSGLT1 inhibitor.

Developing peptide-based fusion inhibitors as an antiviral strategy utilizing coronin 1 as a template.

Enveloped viruses enter the host cells by endocytosis and subsequently fuse with the endosomal membranes, or fuse with the plasma membrane at the cell surface. The crucial stage of viral infection, regardless of the route taken to enter the host cell, is membrane fusion. The present work aims to develop a peptide-based fusion inhibitor that prevents membrane fusion by modifying the properties of the participating membranes, without targeting a protein.

Unveiling the Significance of tert-Butoxides in Transition Metal-Free Cross-Coupling Reactions.

The astounding reactivity of tert-butoxides in transition metal-free coupling reactions is driving the scientific community towards a new era of environmental friendly, as well as cost-effective, transformation strategies. Transition metal-catalyzed coupling reactions generate hazardous wastes and require harsh reaction conditions, mostly at elevated temperature, which increases not only costs but also environmental concerns regarding the methodology. Tert-butoxide-catalyzed/mediated coupling reactions have several advantages and potential applications.

Pemetrexed-loaded supramolecular acetal-functionalized pH-responsive nanocarriers selectively induce apoptosis through biotin receptors to enhance antitumor efficacy.

A novel pH-responsive crystalsomes has been developed using acetal-functionalized pillar[5]arenes (AP[5]) and methyl viologen (MV) through host-guest interactions. The successful synthesis of AP[5] was confirmed via H-NMR spectroscopy, while the formation of the host-guest complex between AP[5] and MV was also verified using ¹H-NMR. The supramolecular assemblies formed at a 1:1 molar ratio of AP[5] to MV exhibited remarkable colloidal stability, a negative surface charge, and a high association constant.

Withaferin A decreases glycolytic reprogramming in breast cancer.

Reprogrammed glucose metabolism is considered as the hallmark of cancer with therapeutic implications. Phytocompounds have potential to inhibit cancer metabolism. Here, we tested the ability of Withaferin A (WA), a withanolide derived from Withania somnifera, in modulating cancer metabolism.

3,5-disubstituted pyridines with potent activity against drug-resistant clinical isolates.

We designed and synthesized a series of compounds with a 3,5-disubstituted pyridine moiety and evaluated them against (Mtb) and drug-resistant Mtb clinical isolates. A library of 3,5-disubstituted pyridine was synthesized. The compounds were screened for activity against H37Rv.

Exploring the Potential of Saffron as a Therapeutic Agent in Depression Treatment: A Comparative Review.

Depression is a significant mental health challenge globally. While traditional antidepressants are effective, they often have unwanted side effects. Saffron, a natural spice derived from L.

ATM1, an essential conserved transporter in Apicomplexa, bridges mitochondrial and cytosolic [Fe-S] biogenesis.

The Apicomplexa phylum encompasses numerous obligate intracellular parasites, some associated with severe implications for human health, including Plasmodium, Cryptosporidium, and Toxoplasma gondii. The iron-sulfur cluster [Fe-S] biogenesis ISC pathway, localized within the mitochondrion or mitosome of these parasites, is vital for parasite survival and development. Previous work on T.

Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant .

In this work, a novel series of naphthalimide hydrazide derivatives were designed, synthesized and evaluated against a bacterial pathogen panel. Most of the compounds were found to exhibit potent antibacterial activity against carbapenem-resistant BAA 1605, with MIC ranging from 0.5 to 16 μg mL.

miR4352b a cross-species modulator of SOSTDC1, targets dual pathway to regulate bone health and fracture healing.

Mutations in SOST can lead to various monogenic bone diseases. Its paralog, SOSTDC1, shares 55 % protein sequence homology and belongs to the BMP antagonist class. Sostdc1-/- mice exhibit distinct effects on cortical and trabecular bone.

Amyloid-like Aggregation Propensities of Metabolites- Homogentisic Acid, N-Acetyl Aspartic Acid and Isovaleric Acid.

The transformation of metabolites into amyloidogenic aggregates represent an intriguing dimension in the pathophysiology of metabolic disorders, including alkaptonuria, canavan disease, and isovaleric acidemia. Central to this phenomenon are the metabolites homogentisic acid (HA), N-acetyl aspartic acid (NAA), and isovaleric acid (IVA), which we found, weave an intricate network of self-assembled structures. Leveraging an array of microscopy techniques, we traced the morphological behavior of these assemblies that exhibit concentration and time-dependent morphological transitions from isolated globules to clustered aggregates.

A novel brominated chalcone derivative as a promising multi-target inhibitor against multidrug-resistant Listeria monocytogenes.

Foodborne pathogens continue to challenge public health due to their ability to cause severe illness and their increasing resistance to current antimicrobial treatments. Listeria monocytogenes is a resilient foodborne pathogen that poses significant risks to vulnerable populations, leading to severe infections and high hospitalization rates. The emergence of antimicrobial-resistant (AMR) strains of L.

Drug response-based precision therapeutic selection for tamoxifen-resistant triple-positive breast cancer.

Breast cancer adaptability to the drug environment reduces the chemotherapeutic response and facilitates acquired drug resistance. Cancer-specific therapeutics can be more effective against advanced-stage cancer than standard chemotherapeutics. To extend the paradigm of cancer-specific therapeutics, clinically relevant acquired tamoxifen-resistant MCF-7 proteome was deconstructed to identify possible druggable targets (N = 150).