Neuroprotective effect of Tozasertib in Streptozotocin-induced alzheimer's mice model.

Alzheimer's disease (AD) is responsible for more than 80% of cases of dementia in senior individuals globally. In the current study, the role of modulation of the FGF1/PI3K/Akt pathway in the protective effect of tozasertib was evaluated. Experimental dementia was induced in mice by injecting streptozotocin (STZ) intracerebroventricularly.

Integrated computational and biological evaluations of newly synthesized thiadiazole-based VEGFR-2 inhibitors with targeted anti-breast cancer activity.

The development of novel VEGFR-2 inhibitors remains a promising strategy for targeted breast cancer therapy, particularly against aggressive triple-negative breast cancer subtype. In this study, a series of thiadiazole derivatives were designed, synthesized, and biologically evaluated for their anti-proliferative activity against MDA-MB-231 and MCF-7 breast cancer cell lines. Among them, compound 7 exhibited superior cytotoxicity (IC₅₀ = 5.

Development of New Thiadiazole Derivatives as VEGFR-2 Inhibitors With Anticancer and Proapoptotic Activities‏.

A series of thiadiazole-based derivatives were synthesized and evaluated for their potential as VEGFR-2 inhibitors and anticancer agents. Among them, compound 7b demonstrated significant cytotoxic activity against MCF-7 breast cancer cells, with an IC value of 6.13 µM, surpassing that of the reference drug sorafenib (IC: 7.

The AMPK/GDF15 Axis: A Novel Target for the Neuroprotective Effects of Metformin in Ischemic Stroke.

Metformin is an anti-diabetic drug used in the management of type 2 diabetes (T2D). Metformin has different pleiotropic effects, such as anti-inflammatory, antioxidant, antithrombotic, and vasculoprotective. Metformin has neuroprotective effects against neurodegenerative diseases and ischemic stroke.

Evaluation of drug interactions in outpatients taking antipsychotic medications.

Introduction: Drug-drug interactions (DDIs) of antipsychotic medications are clinically significant as they can result in toxicity or treatment failure. This study aims to assess the potential drug-drug and drug-tobacco interactions associated with antipsychotic medications in an outpatient setting. Predictors of antipsychotic DDIs and the impact of potential DDIs on patients' clinical outcomes were also evaluated in this study.

Development of new anticancer thiadiazole-sulfonamides as dual EGFR/carbonic anhydrase inhibitors.

Background: Thiadiazole-sulfonamide derivatives were synthesized as dual inhibitors of epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) to develop selective anticancer agents.

Methods: Cytotoxicity was evaluated against MDA-MB-231 and MCF-7 breast cancer cells, with selectivity tested on Vero cells. Enzymatic inhibition studies were conducted against EGFR and CA-IX, using erlotinib and acetazolamide as reference drugs.

New nicotinamide-thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and and evaluation.

Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development. In this study, novel nicotinamide-thiadiazol hybrids were synthesized and evaluated for their anti-breast cancer potential through VEGFR-2 inhibition. The compounds were assessed for their cytotoxicity against MDA-MB-231 and MCF-7 cell lines.

Pharmacogenetics as a Future Tool to Risk-Stratify Breast Cancer Patients According to Chemotoxicity Potential from the Doxorubicin Hydrochloride and Cyclophosphamide (AC) Regimen.

Studying single-nucleotide polymorphisms (SNPs) in xenobiotic-transporting and metabolizing enzyme genes before administering the doxorubicin hydrochloride and cyclophosphamide (AC) regimen may help optimize breast cancer (BC) treatment for individual patients. : Genotyping specific SNPs on genes encoding for the transport and metabolism of the AC regimen and study their association with its chemotherapeutic toxicity. This prospective cohort study was conducted in two hospitals in Egypt.

Design and synthesis of thiadiazoles as anticancer, apoptotic, and VEGFR-2 inhibitors.

Background: Vascular endothelial growth factor receptor (VEGFR-2) inhibitors are critical in cancer therapy due to their role in suppressing tumor angiogenesis. Herein, we report a new series of thiadiazole-based derivatives as potential VEGFR-2 inhibitors with promising anticancer activity.

Methods: The synthesized compounds were evaluated for anti-proliferative activity against human cancer cell lines (HCT-116, MCF-7, and HepG-2), and WI-38 as normal cells.

Evaluating the Use of Inhaled Budesonide and Ipratropium Bromide Combination in Patients at High Risk of Acute Respiratory Distress Syndrome Development: A Randomized Controlled Trial.

There is a scarcity of pharmacological treatments that efficiently address lung injury in individuals experiencing acute respiratory distress syndrome (ARDS). Early inhaled corticosteroids and ipratropium may reduce pulmonary inflammation and injury of the lungs, minimizing the risk of ARDS. This is a double-blinded randomized control trial conducted on patients at risk of ARDS.

Development and Validation of a New Adherence Scale for Antiseizure Medications [ASASM].

The objective was to develop and validate a multidimensional scale that measures adherence levels to antiseizure medications and detects patients' reasons for non-adherence. A new scale was developed, namely the "Adherence Scale for Anti-Seizure Medication(s)-10 items [ASASM-10]". It consists of ten statements that cover different causes of non-adherence to antiseizure medications.

The potential therapeutic role of berberine in treating epilepsy focusing on temporal lobe epilepsy: State of art and ongoing perspective.

Epilepsy is a neurological disease characterized by unprovoked recurrent epileptic seizures. Temporal lobe epilepsy (TLE) is the commonest type of focal epilepsy in adults that resist to the conventional anti-seizure medications (ASMs). Interestingly, ASMs do not affect the epileptogenesis and progression of disease.

Chemical composition, antimicrobial, and antioxidant properties of essential oils from asso. and caball. from Morocco: and evaluation.

Introduction: Morocco is home to a remarkable diversity of flora, including several species from the Artemisia genus. This study aims to thoroughly examine the chemical composition of essential oils derived from Artemisia species and assess their antibacterial and antioxidant properties through in vitro experiments and in silico simulations.

Methods: Samples of Artemisia herba-alba Asso.

Non-Adherence to Antiseizure Medications: Rate and Predictors in Saudi Arabia.

: The objective of this paper is to determine the rate and predictors of non-adherence to antiseizure medications in Saudi Arabia. : A cross-sectional study which involved questionnaires and data collection from patients' medical records was conducted at neurology clinics. The rate of non-adherence to antiseizure medications was measured using "the Medication Adherence Rating Scale" (MARS).

Identification of compounds from and using HPLC/UV-ESI-MS and comparative analysis of their antioxidant, antimicrobial, anticoagulant, and antidiabetic properties.

The aim was to assess the phytochemical composition, phenolic component levels, and biological properties of the flowering tops of and . The study employed phytochemical assays, spectrophotometric techniques for quantitative analysis of polyphenols, flavonoids, and tannins, and compound identification using HPLC/UV-ESI-MS. The antimicrobial, antioxidant, anticoagulant, and antidiabetic properties were examined both and .

Comparative Efficacy of Inhaled and Intravenous Corticosteroids in Managing COVID-19-Related Acute Respiratory Distress Syndrome.

Acute respiratory distress syndrome (ARDS) is a life-threatening condition in which the lungs fail to provide sufficient oxygen to the body's vital organs. It is commonly associated with COVID-19 patients. Severe cases of COVID-19 can lead to lung damage and organ failure due to an immune response in the body.

Investigation of 3-Phenylcoumarin Derivatives as Potential Multi-target Inhibitors for Human Cholinesterases and Monoamine oxidases: A Computational Approach.

Alzheimer's disease (AD) is the predominant etiology of dementia, impacting a global population of approximately 50 million individuals. In the field of medicinal chemistry, there have been notable advancements in the utilization of monoamine oxidase (MAO) and cholinesterase (ChE) inhibitors for the purpose of addressing the neurotransmitter shortage associated with Alzheimer's disease (AD). A selection of previously synthesized 3-Phenylcoumarin derivatives (5a-m) were selected for examination in the pursuit of potential multi-targeting inhibitors of MAO-A, MAO-B, AChE, and BChE.

New Thieno[2,3-d]pyrimidines as Anticancer VEGFR-2 Inhibitors with Apoptosis Induction: Design, Synthesis, and Biological and Studies.

Background: Vascular endothelial growth factor receptor-2 (VEGFR-2) is a critical protein involved in tumor progression, making it an attractive target for cancer therapy.

Objective: This study aimed to synthesize and evaluate novel thieno[2,3-d]pyrimidine analogues as potential anticancer VEGFR-2 inhibitors.

Methods: The thieno[2,3-]pyrimidine analogues were synthesized following the pharmacophoric features of VEGFR-2 inhibitors.

Anti-virulence potential of patuletin, a natural flavone, against and investigations.

is a highly prevalent and aggressive human pathogen causing a wide range of infections. This study aimed to explore the potential of Patuletin, a rare natural flavone, as an anti-virulence agent against . .

Rationale design and synthesis of new apoptotic thiadiazole derivatives targeting VEGFR-2: computational and studies.

This work presents the synthesis and , and analyses of new thiadiazole derivatives that are designed to mimic the pharmacophoric characteristics of vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. A comprehensive evaluation of the inhibitory properties of the synthesized thiadiazole derivatives against the cancer cell lines MCF-7 and HepG2 identified several auspicious candidates. Among them, compound 14 showed remarkably low IC values of 0.

Design, Molecular Modeling, MD Simulations, Essential Dynamics, ADMET, DFT, Synthesis, Anti-proliferative, and Apoptotic Evaluations of a New Anti-VEGFR-2 Nicotinamide Analogue.

Objectives: This study aims to design and evaluate ( and ) a new nicotinamide derivative as an inhibitor of VEGFR-2, a major mediator of angiogenesis Methods: The following studies were performed; DFT calculations, molecular modelling, MD simulations, MM-GBSA, PLIP, and PCAT studies. The compound's (ADMET) analysis was also conducted. Subsequently, the compound ((E)--(4-(1-(2-(4-(4-Chlorobenzamido)benzoyl)hydrazono)ethyl) phenyl)nicotinamide) was successfully synthesized and designated as compound .

Exploring the anticancer properties of a new nicotinamide analogue: Investigations into in silico analysis, antiproliferative effects, selectivity, VEGFR-2 inhibition, apoptosis induction, and migration suppression.

Background: This study focuses on the development and evaluation of (E)-N-(3-(1-(2-(4-bromobenzoyl)hydrazono)ethyl)phenyl)nicotinamide (BHEPN) as a potential inhibitor of Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2).

Methods: Computational investigations as density function theory (DFT), docking, molecular dynamics (MD) simulations, and ADMET) in addition to in vitro (VEGFR-2 inhibition, cytotoxicity against HepG2 and MCF-7 cancer cell lines, selectivity index, cells cycle analysis, apoptosis investigation, and cells migration assay) studies were conducted.

Results: DFT calculations determined the three-dimensional structure and indicated the reactivity of BHEPN.

Discovery of new VEGFR-2 inhibitors and apoptosis inducer-based thieno[2,3-]pyrimidine.

VEGFR-2 is a key regulator of cancer cell proliferation, migration and angiogenesis. Development of thieno[2,3-]pyrimidine derivatives as potential anti-cancer agents targeting VEGFR-2. Seven and nine studies were conducted.

Repurposing of Strychnine as the Potential Inhibitors of Aldo-keto Reductase Family 1 Members B1 and B10: Computational Modeling and Pharmacokinetic Analysis.

AKR1B1 and AKR1B10 are important members of aldo-keto reductase family which plays a significant role in cancer progression by modulating cellular metabolism. These enzymes are involved in various metabolic processes, including the synthesis and metabolism of hormones, detoxification of reactive aldehydes, and the reduction of various endogenous and exogenous compounds. This study aimed to explore the potential of strychnine as an anticancer agent by targeting AKR1B1 and AKR1B10 via drug repurposing approach.