Synthesis of novel pyridine and pyrazolyl pyridine conjugates with potent cytotoxicity against HepG2 cancer cells as PIM-1 kinase inhibitors and caspase activators.

A novel series of nicotinonitrile and pyrazolyl nicotinonitrile were synthesized, and their PIM-1 kinase inhibitors and caspase activators were investigated. New Manich bases 6-8 were synthesized reaction of pyridine 4 with piperidine, dimethyl amine, and morpholine in the presence of formalin. On the other hand, the pyrazolyl analogues 10-12 were synthesized heterocyclization of acetohydrazide derivative 9 with acetylacetone, malononitrile, and ethyl cyanoacetate, respectively, in ethanol.

Correction: Design, synthesis, pharmacological evaluation, and studies of the activity of novel spiro pyrrolo[3,4-]pyrimidine derivatives.

[This corrects the article DOI: 10.1039/D3RA07078F.].

Glycyrrhizin alleviated cisplatin-induced testicular injury by inhibiting the oxidative, apoptotic, hormonal, and histological alterations.

Objective: To evaluate the potential contribution of glycyrrhizin (GLZ) to mitigate the testicular toxicity linked to cisplatin (CIS) intoxication.

Methods: 40 mature male Wistar albino rats (Rattus norvegicus albinus) were randomly divided into 4 equal groups (n = 10) for 60 days: the control group, CIS-treated group (single dose of 7 mg/kg, IP), GLZ-treated group (25 mg/kg, PO), and GLZ plus CIS-treated group. Blood and testis samples were examined using biochemical, histological, and immunohistochemical techniques.

Effects of α-sitosterol on growth, hematobiochemical profiles, immune-antioxidant resilience, histopathological features and expression of immune apoptotic genes of Nile tilapia, Oreochromis niloticus, challenged with Candida albicans.

In this study, the effect of the Streptomyces misakiensis metabolite (α- sitosterol, 0, 20, 40, 60, and 80 mg/kg) dietary supplementation on growth performance, antioxidant-immune stability and Candida albicans resistance of Nile tilapia was evaluated. The results revealed that the incorporation of α-sitosterol at doses of 60 and 80 mg/kg into the diet significantly improved the growth rate of Nile tilapia. The fish receiving 80 mg/kg showed an increased level of high-density lipoprotein, total protein, globulin, and albumin, and significantly reduced levels of indicators of hepato-renal damage, glucose, triglycerides, low-density lipoprotein, and total cholesterol.

FABP4, GINS2 and CBX7 Expression in Cancer Cervix Tissues: Clinical, Pathological and Prognostic Implications.

Background & Objective: Cervical cancer spreads to the pelvic lymph nodes, leading to a high incidence of cancer recurrence and unfavorable survival rates. Therefore, there is an urgent need to detect new predictive biomarkers for the early assessment of pelvic lymph node status in patients with cervical cancer. The current study aimed to assess the expression of FABP4, GINS2, and CBX7 in cervical cancer tissue to detect their prognostic and predictive roles in developing lymph node metastases in patients with that cancer type.

Azole-based compounds as potential anti- agents.

is an opportunistic pathogen with public health implications, largely due to its invasive nature and non-specific symptoms. Our study focuses on the potential of azole compounds, particularly those with triazole scaffolds, as anti-amoebic agents. Out of 10 compounds, compounds T1 and T8 exhibited effective anti- activity with MIC values of 125.

Synthesis of novel bioactive pyrido[2,3-]pyrimidine derivatives with potent cytotoxicity through apoptosis as PIM-1 kinase inhibitors.

Direct synthesis and cytotoxicity activity of new series of pyrido[2,3-]pyrimidine was described. Nicotinamide 2 was synthesized cyclization of -cyclohexyl derivative with cyanoacetamide. The -aminonicotinonitrile 2 was subjected to acylation or thio acylation process followed by intramolecular heterocyclization to afford the desired pyrido[2,3-]pyrimidine (3-10) and pyrido triazine 11.

Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.

Guided by the molecular hybridization principle, a novel series of 4-chloropyridazinoxyphenyl conjugates (3a-h, 4a-e, and 5) was designed and synthesized as proposed apoptotic inducers and PARP-1 inhibitors. The growth inhibition % of the designed hybrids was investigated in eleven cancer cell lines, where the anticancer activities were found to be in the following order: 4-chloropyridazinoxyphenyl-aromatic ketones hybrids (3a-h) > 4-chloropyridazinoxyphenyl-benzyloxyphenylethan-1-one hybrids (4a-e) > 4-chloropyridazinoxyphenyl-thiazolidine-2,4-dione hybrid (5). Further, the most sensitive three cancer cell lines (HNO97, FaDu, and MDA-MB-468) were selected to measure the IC values of the new hybrids.

extract maximizes the efficacy of simvastatin as a hypolipidemic drug in obese male rats.

Obesity became a serious public health problem with enormous socioeconomic implications among the Egyptian population. The present investigation aimed to explore the efficacy of extract as a hypolipidemic agent combined with the commercially well-known anti-obesity drug simvastatin in obese rats. Thirty-five male Wister rats were randomly divided into five groups as follows: group I received a standard balanced diet for ten weeks; high-fat diet was orally administered to rats in groups II-V for ten weeks.

Design, synthesis, pharmacological evaluation, and studies of the activity of novel spiro pyrrolo[3,4-]pyrimidine derivatives.

In the present study, spiro compounds are shown to have distinctive characteristics because of their interesting conformations and their structural impacts on biological systems. A new family of functionalized spiro pyrrolo[3,4-]pyrimidines is prepared the one-pot condensation reaction of amino cyclohexane derivatives with benzaldehyde to prepare fused azaspiroundecanedione and azaspirodecenone/thione derivatives. A series of synthesized spiro compounds were scanned against DPPH and evaluated for their ability to inhibit COX-1 and COX-2.

Novel phenylthiazoles with a -butyl moiety: promising antimicrobial activity against multidrug-resistant pathogens with enhanced ADME properties.

The structure-activity relationship of a new -butylphenylthiazole series, with a pyrimidine linker, was investigated. We wished to expand knowledge of this novel class of antibiotics by generating 21 new derivatives bearing ≥2 heteroatoms in their side chains. Their activity was examined against isolates of methicillin-resistant (MRSA), , , , and .

and studies of -loaded electrospun PLGA/PMMA/collagen nanofibers for accelerating topical wound healing.

This work aims to develop plant extract-loaded electrospun nanofiber as an effective wound dressing scaffolds for topical wound healing. Electrospun nanofibers were fabricated from leaf extract (SCLE), poly(lactic--glycolic acid) (PLGA), poly(methyl methacrylate) (PMMA), collagen and glycine. Electrospinning conditions were optimized to allow the formation of nanosized and uniform fibers that display smooth surface.

Exploitation of multi-walled carbon nanotubes/Cu(ii)-metal organic framework based glassy carbon electrode for the determination of orphenadrine citrate.

Metal organic frameworks (MOFs), with structural tunability, high metal content and large surface area have recently attracted the attention of researchers in the field of electrochemistry. In this work, an unprecedented use of multi-walled carbon nanotubes (MWCNTs)/copper-based metal-organic framework (Cu-BTC MOF) composite as an ion-to-electron transducer in a potentiometric sensor is proposed for the determination of orphenadrine citrate. A comparative study was conducted between three proposed glassy carbon electrodes, Cu-MOF, (MWCNTs) and MWCNTs/Cu-MOF composite based sensors, where Cu-MOF, MWCNTs and their composite were utilized as the ion-to-electron transducers.

Naphthylthiazoles: a class of broad-spectrum antifungals.

Cryptococcal infections remain a major cause of mortality worldwide due to the ability of to pass through the blood-brain barrier (BBB) causing lethal meningitis. The limited number of available therapeutics, which exhibit limited availability, severe toxicity and low tolerability, necessitates the development of new therapeutics. Investigating the antifungal activity of a novel series of naphthylthiazoles provided -diaminocyclohexyl derivative 18 with many advantageous attributes as a potential therapeutic for cryptococcal meningitis.

Protein Expression of NEK2, JMJD4, and REST in Clear Cell Renal Cell Carcinoma (ccRCC): Clinical, Pathological, and Prognostic Findings.

Background & Objective: Cells of renal cell carcinoma (RCC) are resistant to the most currently used chemotherapeutic agents and targeted therapies; hence, we evaluated the expression of NEK2, JMJD4, and REST in cases of clear cell renal cell carcinoma (ccRCC) and benign adjacent tissues of kidney to detect associations between their expression and clinicopathological features, prognostic data, tumor recurrence, and survival rates.

Methods: We collected 200 samples including tumoral and adjacent non-neoplastic tissues related to 100 ccRCC patients. All samples were evaluated for the expression of NEK2, JMJD4, and REST, and the patients were followed up for about 5 years.

Exploring novel aryl/heteroaryl-isosteres of phenylthiazole against multidrug-resistant bacteria.

Antimicrobial resistance has become a concern as a worldwide threat. A novel scaffold of phenylthiazoles was recently evaluated against multidrug-resistant to control the emergence and spread of antimicrobial resistance, showing good results. Several structural modifications are needed based on the structure-activity relationships (SARs) of this new antibiotic class.

Mycotoxins in milk: Occurrence and evaluation of certain detoxification attempts.

Milk contaminated with mycotoxins is a significant issue affecting human health, especially in infants. The current study aimed to investigate the presence of mycotoxins in milk collected from women farmers' vendors (WFV), and to evaluate certain herbal plant fibers as green mycotoxin binders. Moreover, explore the binding efficiency ratios of mycotoxins using shaking or soaking process incorporated with herbal extracts.

Aleppo galls alleviate paracetamol-induced hepatotoxicity and tissue damage: an experimental study.

Background: Acute paracetamol toxicity is a common and potentially life-threatening emergency causing liver failure that may necessitate liver transplantation. Unfortunately, current therapies are still defective.

Objectives: To investigate the protective effects exerted by Aleppo galls (Quercus infectoria Olivier) extract against acute paracetamol toxicity in mice.

Expanding the structure-activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents.

With the continuous and alarming threat of exhausting the current antimicrobial arsenals, efforts are urgently needed to develop new effective ones. In this study, the antibacterial efficacy of a set of structurally related acetylenic-diphenylurea derivatives carrying the aminoguanidine moiety was tested against a panel of multidrug-resistant Gram-positive clinical isolates. Compound 18 was identified with a superior bacteriological profile than the lead compound I.

A prospective randomized controlled study on the role of restoring liver diaphragm surface tension and pain control at port sites in optimizing pain management following laparoscopic cholecystectomy.

Introduction: After laparoscopic cholecystectomy (LC), pain is still a significant concern leading to extended hospital stays or readmissions. A standardized strategy is needed to offer effective pain relief postoperatively. The pain in the early postoperative period is mainly due to elimination of intraperitoneal surface tension.

Efficient selective targeting of CYP51 by oxadiazole derivatives designed from plant cuminaldehyde.

infection represents a global threat with associated high resistance and mortality rate. Azoles such as the triazole drug fluconazole are the frontline therapy against invasive fungal infections; however, the emerging multidrug-resistant strains limit their use. Therefore, a series of novel azole 1-15 derivatives were developed based on a modified natural scaffold to combat the evolved resistance mechanism and to provide improved safety and target selectivity.

Effective corrosion inhibition of mild steel in hydrochloric acid by newly synthesized Schiff base nano Co(ii) and Cr(iii) complexes: spectral, thermal, electrochemical and DFT (FMO, NBO) studies.

Two new cobalt(ii) and chromium(iii) complexes were synthesized and characterized by FT-IR, HNMR, UV, elemental analysis, TGA, conductivity, XRD, SEM, and magnetic susceptibility measurements. Structural analysis revealed a bi-dentate chelation and octahedral geometry for the synthesized complexes. The optical band gap of the Co(ii)-L and Cr(iii)-L complexes was found to be 3.