Synthesis and cytotoxicity evaluation of novel 1,8-acridinedione derivatives bearing phthalimide moiety as potential antitumor agents.

In this study, we aimed to develop hybrid antitumor compounds by synthesizing and characterizing novel N-substituted acrididine-1,8-dione derivatives, designed as hybrids of phthalimide and acridine-1,8-diones. We employed a three-step synthetic strategy and characterized all compounds using IR, 1H NMR, 13C NMR, and LC-MS. The cytotoxicity and antitumor activity of five compounds (8c, 8f, 8h, 8i, and 8L) against four cancer cell lines (H460, A431, A549, and MDA-MB-231) compared to human skin fibroblast cells were evaluated. Among the synthesized compounds, compound 8f showed promising activity against skin and lung cancers, with favorable IC50 values and selectivity index. The relative changes in mRNA expression levels of four key genes (p53, TOP2B, p38, and EGFR) in A431 cells treated with the five synthesized compounds (8c, 8f, 8h, 8i, and 8L) were also investigated. Additionally, molecular docking studies revealed that compound 8f exhibited high binding affinity with TOP2B, p38, p53, and EGFR, suggesting its potential as a targeted anticancer therapy. The results obtained indicate that N-substituted acrididine-1,8-dione derivatives have the potential to be developed as novel antitumor agents with a dual mechanism of action, and compound 8f is a promising candidate for further investigation.

The synthesis and antineoplastic activities of thiaziridine, sulfidometylphosphonium, and dithiaphosphitane-sulfide against the Ehrlich ascites carcinoma.

Phosphonium compounds offer an attractive branch of research that chemists and biologists apply for producing many novel drugs for various applications, and its polymeric ingredients are composed of quaternary ammonium and phosphonium salts. The reactions of isothiocyanate with phosphinimine bestow thiaziridine, carbamate, and thiourea derivatives. Moreover, isothiocyanate reacts with tris (dimethylamino) phosphine leading to the formation of sulfidomethyl phosphonium. Lawesson's and Japanese reagents have potential to react with isothiocyanates to generate dithiaphosphetane sulfides. Treatment of isocyanate with Lawesson' s or Japanese reagents under reflux conditions affords thiaphosphetidinone sulfide, but when applied at room temperature, the dithiaphosphetane sulfide was isolated. Ehrlich ascites carcinoma (EAC) mice model was used to investigate potential anticancer properties of the novel phosphonium and thiophosphate derivatives. Synthesized compounds (100 mg/kg b.w.) were administered orally to the EAC-bearing mice for about 2 weeks. Compounds' antineoplastic activity was determined by the evaluation of volume, viability, and inhibition percent of EAC cells. In addition, DNA fragmentation percent was assessed. The expression of apoptotic marker genes (Bax, Bcl2, Caspase 3) and encoding proinflammatory cytokines (TNF-α) and pro-apoptotic protein (p53) were inspected by real time-quantitative polymerase chain reaction (RT-qPCR). The overall conclusion was based on the findings that treatment with synthesized compounds leads to decrease in tumor volume, increase in tissue DNA fragmentation, downregulation of Bcl2 gene, and upregulation of Bax, caspase3, and p53 markers, along with decrease in TNF-α level in liver tissues. These findings suggest that the anticancer mechanism of these compounds is based on the programmed cell death (Apoptosis).

Seawater Absorption and Adhesion Properties of Hydrophobic and Superhydrophobic Thermoset Epoxy Nanocomposite Coatings.

The enhancement of both thermal and mechanical properties of epoxy materials using nanomaterials becomes a target in coating of the steel to protect it from aggressive environmental conditions for a long time, with reducing the cost. In this respect, the adhesion properties of the epoxy with the steel surfaces, and its proper superhyrophobicity to repel the seawater humidity, can be optimized via addition of green nanoparticles (NPs). In-situ modification of silver (Ag) and calcium carbonate (CaCO3) NPs with oleic acid (OA) was carried out during the formation of Ag-OA and CaCO3-OA, respectively. The epoxide oleic acid (EOA) was also used as capping for Ca-O3 NPs by in-situ method and epoxidation of Ag-OA NPs, too. The morphology, thermal stability, and the diameters of NPs, as well as their dispersion in organic solvent, were investigated. The effects of the prepared NPs on the exothermic curing of the epoxy resins in the presence of polyamines, flexibility or rigidity of epoxy coatings, wettability, and coatings durability in aggressive seawater environment were studied. The obtained results confirmed that the proper superhyrophobicity, coating adhesion, and thermal stability of the epoxy were improved after exposure to salt spray fog for 2000 h at 36 °C.

Methylene Blue Catalytic Degradation Using Silver and Magnetite Nanoparticles Functionalized with a Poly(ionic liquid) Based on Quaternized Dialkylethanolamine with 2-Acrylamido-2-methylpropane Sulfonate-co-Vinylpyrrolidone.

Catalytic degradation of organic water pollutants has emerged as a cost- and energy-effective technique to treat wastewater. In this work, new silver and magnetite nanoparticles (NPs) were prepared with a protic poly(ionic liquid) (PIL) based on a quaternized diethylethanolamine cation combined with 2-acrylamido-2-methylpropane sulfonate-co-vinylpyrrolidone (QAMPSA/VP) as a capping and a reducing agent. The morphology, particle size, surface charge, thermal stability, and magnetic properties of QAMPS/VP-Ag and Fe3O4 NPs were investigated to determine the efficiency of the PIL as a reducing and a capping agent to protect the produced NPs from oxidation or thermal degradation. The activation energy, enthalpy, and entropy of the catalytic degradation of the cationic methylene blue (MB) dye in the presence of QAMPS/VP-Ag and Fe3O4 NPs were determined. The data elucidated that MB was completely degraded in 8 min in the presence of QAMPS/VP-Fe3O4 NPs as a Fenton oxidation catalyst. Moreover, their good magnetic properties allowed their easy separation and reuse for five cycles without losing their magnetic or catalytic properties.

Synthesis of New Magnetic Crosslinked Poly (Ionic Liquid) Nanocomposites for Fast Congo Red Removal from Industrial Wastewater.

Advanced materials reliant on cross-linked magnetic poly (ionic liquids) (PILs) have been widely utilized in environmental applications for water purification. The present work demonstrates our preparation of a new magnetic cross-linked PIL based on quaternized 4-vinyl-pyridine-co-acrylamide (QVP/AAm). The chemical composition, thermal stability, magnetic properties, morphology, particle sizes, and zeta potential of the magnetic QVP/AAm composites were investigated. Fast adsorption and desorption kinetics, high adsorption capacity, rapid magnetic separation, and the absence of secondary pollution in the adsorption process make QVP/AAm-Fe3O4 a highly effective adsorbent for the elimination of anionic acidic Congo red contaminants from industrial wastewater.

Novel Magnetic Silica-Ionic Liquid Nanocomposites for Wastewater Treatment.

In this work, new imidazolium silica-ionic liquids doped with magnetite nanocomposites are prepared for use in the field of water purification owing to their unique properties, which can be manipulated by an external magnetic field. A silane precursor based on aminopropyltriethoxysilane (APTS) condensed with p-hydroxybenzaldehyde and glyoxal in an acetic acid solution is used to prepare disiloxyimidazolium ionic liquid (SIMIL). The silica composite (Si-IL) and silica-coated magnetite (Fe3O4-Si-IL) composites are prepared using the sol-gel technique. The chemical structures, morphologies, crystalline lattice structures, thermal stabilities, surface charges, surface areas, particle sizes, and magnetic characteristics of Fe3O4-Si-IL and Si-IL are investigated. The Fe3O4-Si-IL and Si-IL nanocomposites show excellent chemical adsorption capacities as 653 and 472 mg g-1, respectively, during times ranging 90 to 110 min when they are used as adsorbents to remove Congo red (CR) dye as a water pollutant.

Data on photo-nanofiller models for self-cleaning foul release coating of ship hulls.

The data presented in this article are related to the research article entitled "Smart photo-induced silicone/TiO2 nanocomposites with dominant [110] exposed surfaces for self-cleaning foul-release coatings of ship hulls" (Selimet al., 2016) [1]. This article reports on successfully designing and controlling TiO2 spherical single crystal photo-nanofillers and indicating evidence of fouling resistance after stimulation through UV radiation exposure. These data also reveal that the influence of well-dispersed spherical TiO2 nanoparticles (NPs) into the polymer matrix surface features on the prepared fouling release (FR) coating. Single crystal TiO2 nanospheres have played a large role in the scenario of photocatalysis due to its cost effectiveness, inert nature and photo stability. The model output and the surface and mechanical behavior data of the fabricated UV-irradiated silicone-based FR nanocoatings are made publicly available through analyzing nanocomposite topology, superhydrophilicity and self-cleaning efficiency in order to enable critical analysis of the tailored model. It also investigates the photo-bactericidal effect confirmed through biofilm coverage data disability. The modeled nanocomposites were subjected to comparable studies with other published models so as to understand how different UV-irradiated nano-scale parameters propagate and affect bulk film response.

Synthesis and antiproliferative activity of novel polynuclear heterocyclic compounds derived from 2,3-diaminophenazine.

2,3-Diaminophenazine 1 was used as a precursor for the preparation of some novel phenazine derivatives such as imidazo[4,5-b]phenazine-2-thione 2, its methylthio 3, ethyl 1-aryl-3H-[1,2,4]triazolo[2,3-a]imidazo[4,5-b]phenazines 8a-c, ethyl (2Z)-[3-aminophenazin-2-yl)amino](phenylhydrazono)ethanoate 9, pyrazino[2,3-b]phenazine derivatives 10, 12, 15-17, [1,4]diazepino[2,3-b]phenazine derivatives 13, 14, 2,3-dibenzoylaminophenazine 18, 1H-Imidazo[4,5-b]phenazine derivatives 20, 23a-c, 24, 25 and 4-[(E)-(3-amino phenazin-2-yl)diazenyl] derivatives 27-29. All compounds were tested as inhibitors of the proliferation of human lung carcinoma and colorectal cancer cell lines through inhibition of Tyrosine Kinases. Most of compounds exert good activity against the two cancer cell lines. Five compounds (1, 2, 3, 25 and 28) were found to possess the same activity as the standard drug Cisplatin.

Conversion of 3-arylazo-5-phenyl-2(3H)-furanones into other heterocycles of anticipated biological activity.

3-arylazo-5-phenyl-2(3H)-furanones 3 were prepared and converted into a variety of heterocyclic systems of synthetic and biological importance. Hydrazine hydrate reacted with furanones as nucleophiles and gave the corresponding acid hydrazides 4. The latter products were used as starting materials for the synthesis of 1,3,4-oxadiazoles 6, 9, and the 1,2,4-triazoles 8. Evaluation of the antiviral activity of selected compounds obtained was performed using two viruses: HAV and HSV-1. Some of the tested compounds showed promising activities.

Conversion of some 2(3H)-furanones bearing a pyrazolyl group into other heterocyclic systems with a study of their antiviral activity.

3-(1,3-diphenylpyrazol-4-yl-methylene)-5-aryl-2(3H)-furanones 2 were prepared and converted into a variety of heterocyclic systems of synthetic and biological importance. Benzylamine reacted with the furanones 2; the product was found to depend on the reaction conditions. Thus, at room temperature the open-chain N-benzylamides 3 were obtained, whereas under refluxing conditions the 2(3H)-pyrrolones were obtained. Hydrazine hydrate affected ring opening of the furanones to give the corresponding acid hydrazides 5. The latter products were used as key starting materials for the synthesis of pyridazinones 7 and 8, 1,3,4-oxadiazoles 11 and 13 and 1,2,4-triazoles 12 and 14 all bearing pyrazolyl moiety as a side-chain. Evaluation of antiviral activity of selected examples of the compounds obtained was performed using two viruses: HAV and HSV-1. Some of the tested compounds showed promising activities.