evaluation of novel synthetic pyrazolones as CDK9 inhibitors with enhanced pharmacokinetic properties.

The structural optimization of our recently reported CDK9 inhibitor to furnish novel aminopyrazolones and methylpyrazolones with improved pharmacokinetics. The synthesis of the targeted compounds was accomplished via conventional, grinding and microwave-assisted processes. The cytotoxicity of them was assayed against three carcinomas.

Fusarium verticillioides pigment: production, response surface optimization, gamma irradiation and encapsulation studies.

Background: Natural pigments are becoming more significant because of the rising cost of raw materials, pollution, and the complexity of synthetic pigments. Compared to synthetic pigments, natural pigments exhibit antimicrobial properties and is less allergic. Pigments from microbial sources could easily be obtained in an inexpensive culture media, produced in high yields, and microbes are capable of producing different colored pigments.

pH-Sensitive doxorubicin delivery using zinc oxide nanoparticles as a rectified theranostic platform: anti-proliferative, apoptotic, cell cycle arrest and radio-distribution studies.

Despite enormous advancements in its management, cancer is the world's primary cause of mortality. Therefore, tremendous strides were made to produce intelligent theranostics with mitigated side effects and improved specificity and efficiency. Thus, we developed a pH-sensitive theranostic platform composed of dextran immobilized zinc oxide nanoparticles, loaded with doxorubicin and radiolabeled with the technetium-99m radionuclide (Tc-labelled DOX-loaded ZnO@dextran).

Speciation of vanadium and the interacted solid surface of δ-alumina adsorbent in aqueous media in presence of humic acid.

Speciation of vanadium elements in the presence of δ-alumina in aqueous media was studied to simulate the environmental impact of soil/sediment-water interacted system. Factors affecting this process are pH, presence of humic acid, and δ-alumina concentrations as an abundant sediment/soil components. Different species of both vanadium and surface of δ-alumina were deduced theoretically using MintaqA2 programme.

A prototype system for the removal of Cs from liquid radioactive waste using reverse osmosis membrane.

Cesium removal from aqueous solutions of radioactive waste streams is a challenge in the field of radioactive waste management; this is due to the small atomic radii of Cs metal ions and their high migration ability. So, the development of a withstand system for the removal of Cs is crucial. In the current study, the removal of radioactive cesium from aqueous solutions using an RO-TLC membrane was studied.

Potential production of Ac-225 at Egyptian second research reactor (ETRR-2) through neutron induced transmutation of Ra-226.

A considerable focus has been paid to the production of Ac due to its effective therapeutic action in alpha-targeted radiotherapy. Considering the future global clinical demand, it is necessary to increase the production capacity of Ac. A feasibility study was conducted to investigate the production of Ac through neutron induced transmutation of Ra at the Egyptian Second Research Reactor (ETRR-2) using the MCNPX code.

Analytical study and real simulation for improving the safety of ageing nuclear facility using UPFC.

This paper aims to increase the performance and improve the safety of an ageing Nuclear Facility (NF). Good power quality extends the life of electrical equipment at NF and thus protects it from premature aging. The first stage of this paper presents a measurement and analysis of various power quality events for a real-world case of a NF under different conditions of operation.

Novel radioiodinated desvenlafaxine-loaded lipid nanocapsule for brain delivery.

Lipid nanocapsules (LNCs) are lipid nanocarriers developed for drug delivery enhancement. The antidepressant drug desvenlafaxine (DSV) was entrapped in LNC to improve its brain delivery. Different DSV-loaded LNCs formulae using different oils and surfactants were studied to obtain the optimum formula for further studies.

Multi-functionalization of reduced graphene oxide nanosheets for tumor theragnosis: Synthesis, characterization, enzyme assay, in-silico study, radiolabeling and in vivo targeting evaluation.

Background: In this study, a combination of nanotechnology, organic synthesis and radiochemistry were utilized in order to design an efficient nano-system conjugated with a suitable radionuclide and an antitumor agent for possible application as tumor theragnostic agent.

Method: Four novel compounds (3 and 4a-c) bearing tetrahydroquinazoline-7-sulfonohydrazide or 1,2,3,4-tetrahydroquinazoline-7-sulfonamide scaffold were designed. Then, docking study predicted that the compounds can be considered as potential inhibitors for PARP-1.

Green synthesis, radioiodination and in vivo biodistribution of 5-(2-hydroxyphenyl)-2,4-dihydro-3H-pyrazol-3-one derivatives as potential candidates for lung imaging.

Lung targeting was developed by synthesising pyrazolone derivatives 6a-f under solvent-free and thermal conditions by reacting azo coumarins 4a-c with hydrazines 5a and b using maltose as a biodegradable catalyst. Different spectral data characterized the synthesized agents as proton-NMR, FT-IR, and mass spectra. Direct radioiodination with iodine-131 was performed and optimized to reach the highest radiochemical purities (92 ± 0.

New Thiophenyl-pyrazolyl-thiazole Hybrids as DHFR Inhibitors: Design, Synthesis, Antimicrobial Evaluation, Molecular Modeling, and Biodistribution Studies.

The antibiotic resistance problems constitute a considerable threat to human health worldwide; thus, the discovery of new antimicrobial candidates to conquer this issue is an imperative requirement. From this view, new thiophenyl-pyrazolyl-thiazole hybrids were synthesized and screened for their antibacterial efficiency versus Gram - and Gram + bacterial strains compared to the reference drug amoxicillin. It was noticed that the new hybrids displayed significant antibacterial efficacy versus Gram - bacteria, especially against .

The Development and Validation of Radiopharmaceuticals Targeting Bacterial Infection.

The International Atomic Energy Agency organized a technical meeting at its headquarters in Vienna, Austria, in 2022 that included 17 experts representing 12 countries, whose research spanned the development and use of radiolabeled agents for imaging infection. The meeting focused largely on bacterial pathogens. The group discussed and evaluated the advantages and disadvantages of several radiopharmaceuticals, as well as the science driving various imaging approaches.

Radiological assessment of different monazite grades after mechanical separation from black sand.

In Egyptian black sands, monazite is a precious mineral characterized by its composition, which includes crucial constituents such as thorium, trace amounts of uranium, and rare earth elements. It is essential to evaluate and quantify the extent of gamma-ray exposure resulting from the presence of primordial radionuclides. This necessity arises from human activities that extract and retrieve raw materials in uranium and thorium mining operations.

Sonophoresis-assisted transdermal delivery of antimigraine-loaded nanolipomers: Radio-tracking, histopathological assessment and in-vivo biodistribution study.

Migraine is a disabling neurovascular polygenic disorder affecting life quality with escorted socioeconomic encumbrances. Herein, we investigated the consolidated amalgamation of passive lipomer approach alongside active sonophoresis assisted transdermal delivery of zolmitriptan (ZT) using high frequency ultrasound pre-treatment protocol to mitigate migraine attacks. A modified nanoprecipitation technique was utilized to prepare zolmitriptan loaded lipomers (ZTL) adopting 2 factorial design.

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by Tc radiolabeling technique.

Zolmitriptan (ZT) is a potent second generation triptan, commonly administered to alleviate migraine attacks. ZT suffers various limitations; massive hepatic first pass metabolism, P-gp efflux transporters susceptibility, and limited (≈40%) oral bioavailability. Transdermal route of administration could be explored to enhance its bioavailability.

Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation.

Purpose: The research objective is to design intranasal brain targeted CLZ loaded lecithin based polymeric micelles (CLZ- LbPM) aiming to improve central systemic CLZ bioavailability.

Methods: In our study, intranasal CLZ loaded lecithin based polymeric micelles (CLZ- LbPM) were formulated using soya phosphatidyl choline (SPC) and sodium deoxycholate (SDC) with different CLZ:SPC:SDC ratios via thin film hydration technique aiming to enhance drug solubility, bioavailability and nose to brain targeting efficiency. Optimization of the prepared CLZ-LbPM using Design-Expert® software was achieved showing that M6 which composed of (CLZ:SPC: SDC) in respective ratios of 1:3:10 was selected as the optimized formula.

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, optimization, cytotoxicity & biodistribution utilizing radioiodinated zopiclone.

Nano-structured lipid carriers containing zopiclone were prepared as a targeted drug delivery system to convey zopiclone directly to brain nasal route. Nano-structured lipid carriers were constructed adopting hot emulsification-ultrasonication method using palmitic acid in place of the solid lipid, cod liver oil as liquid lipid, and poloxamer 407 as a surfactant. A three-factor three-level central composite face-centered design was used to optimize the formulated nano-structured lipid carriers.

Computational, in vitro and radiation-based in vivo studies on acetamide quinazolinone derivatives as new proposed purine nucleoside phosphorylase inhibitors for breast cancer.

The present work describes a quinazolinone-based lead optimization for the development of novel purine nucleoside phosphorylase (PNP) inhibitors with quinazolinone scaffold. Nineteen compounds were proposed and docked against PNP, the best 14 compounds with highest docking and affinity scores and low RMSD values were synthesized. Synthesis of new quinazolinone derivatives with variable acetamide substituents on two positions on quinazoline ring was performed.

Adsorption of Co(II) and Eu(III) radionuclides by a sustainable nanobentonite@sodium alginate@oleylamine nanocomposite.

A sustainable and efficient nanobentonite@sodium alginate@oleylamine (Nbent@Alg@OA) nanocomposite has been successfully synthesized via coating reaction of nanobentonite (Nbent) with alginate (Alg) and oleylamine (OA). The nanocomposite has been characterized and examined for the adsorption of Co(II) and Eu(III) radionuclides from simulated radioactive waste solution. FT-IR, XRD, SEM, and HR-TEM techniques have been applied to confirm the structural and morphological characteristics of the Nbent@Alg@OA nanocomposite.

New 5-Aryl-1,3,4-Thiadiazole-Based Anticancer Agents: Design, Synthesis, In Vitro Biological Evaluation and In Vivo Radioactive Tracing Studies.

A new series of 5-(4-chlorophenyl)-1,3,4-thiadiazole-based compounds featuring pyridinium (), substituted piperazines (), benzyl piperidine (), and aryl aminothiazoles () heterocycles were synthesized. Evaluation of the cytotoxicity potential of the new compounds against MCF-7 and HepG2 cancer cell lines indicated that compounds and displayed the highest activity toward the tested cancer cells. A selectivity study demonstrated the high selective cytotoxicity of and towards cancerous cells over normal mammalian Vero cells.

A new modality in targeted delivery of epirubicin for tumor theranosis based on PEGylated silver nanoparticles: Design, radiolabeling and bioevaluation.

This work highlights boosting the tumor targeting efficiency of epirubicin through loading on a new radionanosystem, based on the effective role of silver nanoparticles (AgNPs). Accordingly, PEGylated silver nanoparticles (PEG/AgNPs) were prepared in a size of 20.2 ± 0.

Post-irradiation physicochemical features of polymer composite for the removal of Co(II) and Nd(III) from aqueous solutions.

The scientific impact of this work is the protection of the environment from hazardous pollutants. Gamma irradiation was employed for the preparation of a new composite polymer by irradiating a mixture containing polyvinyl pyrrolidone (PVP), hydroxyethyl methacrylate (HEMA), and tannic acid (TA) to produce PVP-HEMA-TA. The sorption efficiency and capacity of PVP-HEMA-TA were evaluated by studying some factors affecting the sorption of Nd(III) and Co(II) from aqueous solutions.

Optimization, purification, and structure elucidation of anthraquinone pigment derivative from Talaromyces purpureogenus as a novel promising antioxidant, anticancer, and kidney radio-imaging agent.

This study aims to investigate the bioproduction and prospective biological applications of a natural red pigment from Talaromyces purpureogenus AUMC2603. Maximum pigment yield was achieved by a numerical optimization at pH 6, temperature 25 °C, and an 18-day incubation period on Yeast Malt Broth (YMB) media. The crude pigment was separated and purified into two pigment fractions via solid-phase extraction and then characterized as anthraquinone (dominant) and herquinone by LC/MS and HNMR analysis.

Radiolabeling and cytotoxicity of monoclonal antibody Isatuximab functionalized silver nanoparticles on the growth of multiple myeloma.

The goal of this article was to develop a new therapeutic strategy based on nanotechnology for multiple myeloma (MM) treatment which shows a synergism of different mechanisms. In this concern, 12.9 nm-sized silver nanoparticles (AgNPs) were prepared and functionalized with Isatuximab, anti-MM monoclonal antibody (mAb).

A novel β-cyclodextrin/alginate-combined-nickel oxide nanosorbent for adsorptive remediation of Cr and Mn radionuclides.

A Promising nanocomposite from β-Cyclodextrin/Alginate (β-CD/Alg) composite impregnated with nickel oxide nanoparticles (NiO) has been synthesized and characterized using diverse techniques like FT-IR, XRD, TGA, and SEM. The new nanocomposite has been investigated for the efficient remediation of Cr and Mn radionuclides from simulated contaminated radioactive water. All the controlling experimental parameters such as solution pH, contact time, initial radionuclides concentration and adsorbent mass have been investigated and optimized.