Design and synthesis of new 1,2,3-triazole derivatives as VEGFR-2/telomerase downregulatory candidates endowed with apoptotic potential for cancer treatment.

In this current work, we dedicated efforts to designing and synthesizing new 1,2,3-triazole-analogues (5a-d), (6a-d), and (7a-c) to act as dual VEGFR-2 and telomerase inhibitors with promising apoptotic potential. The synthesized analogues were examined against eleven diverse types of cancer cells and two normal cells to assess their ability to inhibit cell growth (GI%). Obviously, compound 7b showed the best average GI% (75.

Dual EGFR and telomerase inhibitory potential of new triazole tethered Schiff bases endowed with apoptosis: design, synthesis, and biological assessments.

Many cancers have displayed resistance to chemotherapeutic drugs over the past few decades. EGFR has emerged as a leading target for cancer therapy inhibiting tumor angiogenesis. Besides, studies strongly suggest that blocking telomerase activity could be an effective way to control the growth of certain cancer cells.

Exploring 1,2,3-triazole-Schiff's base hybrids as innovative EGFR inhibitors for the treatment of breast cancer: In vitro and in silico study.

EGFR inhibitors are a class of targeted therapies utilized in the management of certain tumor kinds such as NSCLC and breast cancer. Series of 1,2,3-triazole-Schiff's base hybrids were designed, synthesized, and estimated for their antitumor effect toward breast cancer cells, MCF-7 and MDA-MB-231. The safety and selectivity of the new compounds were tested using normal cell (WI-38).

Molecular Signaling Pathways of Quercetin in Alzheimer's Disease: A Promising Arena.

Alzheimer's disease (AD) is a neurodegenerative disease characterized by cognitive impairment and memory deficit. Even with extensive research and studies, presently, there is no effective treatment for the management of AD. Besides, most of drugs used in the treatment of AD did not avert the AD neuropathology, and the disease still in a progressive status.

Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation.

VEGFR2 inhibition has been established as a therapeutic approach for managing cancer. A series of curcumin-based analogues were designed, synthesized, and screened for their anticancer activity against MCF-7 and HepG-2 cell lines and WISH normal cells. Compounds 4b, 4d, 4e, and 4f showed potent cytotoxicity against MCF-7 with IC values of 0.

Performance of self-cured versus light-cured universal adhesive in patients with non-carious cervical lesions: 18-month randomized clinical trial.

Objective: To evaluate the clinical performance of self versus light-cured universal adhesive in non-carious cervical lesions (NCCLs) after 18 months.

Materials And Methods: Sixty-eight NCCLs in 28 patients were divided into two equal groups; G1: self-cured universal adhesive (Palfique,Tokuyama,Japan) and G2: light-cured universal adhesive (Single Bond Universal,3 M ESPE,USA). Nanohybrid resin composite (Z350XT, 3 M ESPE, USA) was used as a final restoration.

Item response theory analysis of daytime sleepiness as a symptom of obstructive sleep apnea.

Obstructive sleep apnea (OSA) is a sleep disorder which is linked to many health risks. The gold standard to evaluate OSA in clinical trials is the Apnea-Hypopnea Index (AHI). However, it is time-consuming, costly, and disregards aspects such as quality of life.

Evaluation of covariate effects in item response theory models.

Item response theory (IRT) models are usually the best way to analyze composite or rating scale data. Standard methods to evaluate covariate or treatment effects in IRT models do not allow to identify item-specific effects. Finding subgroups of patients who respond differently to certain items could be very important when designing inclusion or exclusion criteria for clinical trials, and aid in understanding different treatment responses in varying disease manifestations.

Bleeding Outcomes in Patients Treated With Asundexian in Phase II Trials.

Background: Phase II trials of asundexian were underpowered to detect important differences in bleeding.

Objectives: The goal of this study was to obtain best estimates of effects of asundexian vs active control/placebo on major and clinically relevant nonmajor (CRNM) and all bleeding, describe most common sites of bleeding, and explore association between asundexian exposure and bleeding.

Methods: We performed a pooled analysis of 3 phase II trials of asundexian in patients with atrial fibrillation (AF), recent acute myocardial infarction (AMI), or stroke.

Norepinephrine boluses for the prevention of post-reperfusion syndrome in living donor liver transplantation: A prospective, open-label, single-arm feasibility trial.

Background And Aims: Post-reperfusion syndrome (PRS) is a serious haemodynamic event during liver transplantation (LT), which increases early graft dysfunction and mortality. This study aimed to test the efficacy and safety of norepinephrine (NE) boluses to prevent PRS during orthotopic LT.

Methods: This feasibility phase II trial prospectively recruited a single arm of 40 patients undergoing living donor LT.

2-Phenylquinazolin-4(3H)-one scaffold as newly designed, synthesized VEGFR-2 allosteric inhibitors with potent cytotoxicity through apoptosis.

New derivatives of 2-phenylquinazolin-4(3H)-one were designed, synthesized, and biologically evaluated as potent allosteric kinase inhibitors with in situ cytotoxicity against MCF-7 and HepG2 cells. Compounds 15 and 18 among the proposed compounds showed promising antiproliferative activity against MCF-7 (IC = 1.35 µM) and HepG2 cells (IC  = 3.

Enhancement of Neprilysin Activity by Natural Polyphenolic Compounds and Their Derivatives in Cultured Neuroglioma Cells.

The onset of Alzheimer's disease (AD) is characterized by accumulation of amyloid β peptide (Aβ) in the brain. Neprilysin (NEP) is one of the major Aβ-degrading enzymes. Given findings that NEP expression in the brain declines from the early stage of AD before apparent neuronal losses are observed, enhancement of NEP activity and expression may be a preventive and therapeutic strategy relevant to disease onset.

The Relationship Between Acne Vulgaris and Insulin Resistance.

Acne vulgaris is a chronic inflammatory disease of the pilosebaceous unit that usually affects adolescents. The aetiology and severity of acne may be influenced by hyperinsulinemia and insulin resistance. A case-control study was conducted in the dermatology outpatient clinic of Al-Fayhaa Teaching Hospital in Basrah city.

Accuracy of high definition near infrared transillumination camera in detection of hidden proximal caries.

Background: Early caries detection became mandatory in modern dentistry. However, the traditional methods in caries detection had many limitations. Hence,a novel approach based on Near Infrared technology was introduced to overcome such limitations.

Mannitol for prevention of acute kidney injury after liver transplantation: a randomized controlled trial.

Background: Acute kidney injury (AKI) is a common complication after liver transplantation, which is associated with increased morbidity and mortality. Therefore, this study investigated mannitol as an oxygen-free radical scavenger and its role in the prevention of early AKI after living donor liver transplantation (LDLT).

Methods: A total of 84 adult patients who underwent LDLT were randomly assigned to two equal groups: the M group, where patients received 1 g/kg mannitol 20%, or the S group, where patients received an equal volume of saline.

Intraoperative Optic Nerve Sheath Diameter as a Predictor of Early Tacrolimus Neurotoxicity after Living Donor Liver Transplantation.

Background: During liver transplantation, graft reperfusion triggers cerebral hyperemia, increases intracranial pressure, and disrupts the blood-brain barrier, thereby increasing the risk for immunosuppression neurotoxicity. Therefore, we tested the intraoperative optic nerve sheath diameter (ONSD) for predicting tacrolimus neurotoxicity after liver transplantation.

Basic Procedures: We prospectively included 100 adult patients who underwent living donor liver transplantation.

Baseline clusters and the response to positive airway pressure treatment in obstructive sleep apnoea patients: longitudinal data from the European Sleep Apnea Database cohort.

Introduction: The European Sleep Apnea Database was used to identify distinguishable obstructive sleep apnoea (OSA) phenotypes and to investigate the clinical outcome during positive airway pressure (PAP) treatment.

Method: Prospective OSA patient data were recruited from 35 sleep clinics in 21 European countries. Unsupervised cluster analysis (anthropometrics, clinical variables) was performed in a random sample (n=5000).

Design and Synthesis of Coumarin Derivatives as Cytotoxic Agents through PI3K/AKT Signaling Pathway Inhibition in HL60 and HepG2 Cancer Cells.

In this study, a series of coumarin derivatives, either alone or as hybrids with cinnamic acid, were synthesized and evaluated for their cytotoxicity against a panel of cancer cells using the MTT assay. Then, the most active compounds were inspected for their mechanism of cytotoxicity by cell-cycle analysis, RT-PCR, DNA fragmentation, and Western blotting techniques. Cytotoxic results showed that compound () had a significant cytotoxic effect against HL60 cells (IC = 8.

How Internet Websites Portray Herbal Vitality Products Containing : An Evaluation of the Quality and Risks of Online Information.

Background: Tongkat Ali (TA) or is a herbal medicine (HM) plant traditionally used to treat sexual dysfunction and enhance libido in men. Websites containing information about HM are abundant. However, studies have shown that in general the quality of websites containing information on HM is low.

First randomized evaluation of safety, pharmacodynamics, and pharmacokinetics of BAY 1831865, an antibody targeting coagulation factor XI and factor XIa, in healthy men.

Background: Bleeding is a clinically significant issue with all current anticoagulants. Safer antithrombotic strategies are required.

Objectives: To investigate the safety, pharmacodynamics, and pharmacokinetics of BAY 1831865, a humanized, factor XI (FXI)-directed monoclonal antibody, after single intravenous (i.

Clinical effectiveness of high definition fluorescence camera in detection of initial occlusal caries.

Background: Although visual inspection is the preferred route in everyday clinical practise for detecting early caries lesions, novel technologies like light fluorescence-based devices (Vista Proof iX HD smart) have been developed to enhance early caries detection.

Material And Methods: Occlusal surface of 45 molar and 49 premolar teeth from 34 adult participants who fulfilled the eligibility criteria were examined by two observers using three diagnostic methods. Examination was performed visually using the International Caries Detection and Assessment System (ICDAS-II) followed by Vista Proof.

Hepatocellular Carcinoma in Hepatitis C-Related Cirrhosis: Are Advanced Glycation End Products a Key Driver?

Background And Purpose: The advanced glycation end products (AGEs) have been implicated in different diseases' pathogenesis, but their role in hepatocellular carcinoma (HCC) is still a matter of debate. This study aims to investigate the association of AGEs with HCC development in patients with hepatitis C-related cirrhosis.

Methods: Only 153 of the 181 non-diabetic patients with cirrhosis were consecutively involved in this pilot cohort prospective study, along with 34 healthy control participants.

Accuracy of the Light-induced Fluorescent Intraoral Camera in Occlusal Caries Detection.

Aim And Objective: This study was conducted to evaluate the accuracy of a light-induced fluorescence intraoral camera vs the visual-tactile assessment method according to the modified International caries detection and assessment system-II (ICDAS-II) criteria clinically in the detection of initial occlusal caries.

Materials And Methods: Occlusal surfaces of 260 molar and premolar teeth from 52 adult participants were examined by two calibrated observers, using two diagnostic methods. Teeth were initially assessed visually according to the criteria of the ICDAS-II, and then by fluorescence camera (Soprolife®).

First evaluation of the safety, pharmacokinetics, and pharmacodynamics of BAY 2433334, a small molecule targeting coagulation factor XIa.

Background: Coagulation factor XI (FXI) contributes to the development of thrombosis but appears to play a minor role in hemostasis and is, therefore, an attractive anticoagulant drug target.

Objectives: To evaluate the safety, pharmacokinetic, and pharmacodynamic properties of BAY 2433334, an orally administered small molecule targeting activated FXI (FXIa), in healthy men.

Patients/methods: This phase 1 study was conducted in two parts.

Influence of Nanocoats on the Physicomechanical Properties and Microleakage of Bulk-fill and Resin-modified Glass Ionomer Cements: An Study.

Aim: To analyze the impact of two nanocoating materials, EQUIA Forte nanocoat and universal adhesive, on flexural strength, color changes, surface roughness, and microleakage of bulk-fill and resin-modified glass ionomer cements (RM-GICs).

Materials And Methods: A total of 45 specimens were prepared for each group, bulk-fill (EQUIA Forte Fil) and RM-GI (Fuji II LC) cements, according to manufacturer's instructions for flexural strength, color change, and surface roughness tests. Each group was equally subdivided into three subgroups according to coating materials used; either without a coat (negative control) or covered with EQUIA Forte coat or universal adhesive.