Design, Synthesis, Pharmacological Evaluation of Quinazolin-4(3)-Ones Bearing Urea Functionality as Potential VEGFR-2 Inhibitors.

Background: In response to the urgent need for continuous discovery of new anti-proliferative agents, a new series of quinazoline compounds was prepared.

Methods: As a reference, four cancer cell lines-HCT116, HePG2, Hela, and MCF-7-and sorafenib (SOR) were used to assess the novel motifs' in vitro anticancer efficacy. The most cytotoxic compounds were tested in a VEGFR-2 suppressive test and flow cytometric test.

-Alkylated quinazolin-4(3)-ones as dual EGFR/VEGFR-2 kinases inhibitors: design, synthesis, anticancer evaluation and docking study.

Dual targeting by a single molecule has emerged as a promising strategy for fighting cancer. In this study, a new set of 2-thioquinazolin-4(3)-ones as potential anti-cancer surrogates endowed with dual EGFR/VEGFR-2 kinases inhibitory activities were synthesized. The anti-tumor potency of the newly synthesized candidates 4-27 was evaluated against a panel of four cancer cell lines.

Identification of Benzothiazoles Bearing 1,3,4-Thiadiazole as Antiproliferative Hybrids Targeting VEGFR-2 and BRAF Kinase: Design, Synthesis, BIO Evaluation and In Silico Study.

Cancer remains a leading cause of death worldwide, often resulting from uncontrolled growth in various organs. Protein kinase inhibitors represent an important class of targeted cancer therapies. Recently, the kinases BRAF and VEGFR-2 have shown synergistic effects on tumor progression.

Synthesis, bioactivity assessment, molecular docking and ADMET studies of new chromone congeners exhibiting potent anticancer activity.

In consideration of the chromones' therapeutic potential and anticancer activity, a new series of chromanone derivatives have been synthesized through a straightforward reaction between 6-formyl-7-hydroxy-5-methoxy-2-methylchromone (2) and various organic active compounds. The cytotoxic activity of the newly synthesized congeners was investigated against MCF-7 (human breast cancer), HCT-116 (colon cancer), HepG2 (liver cancer), and normal skin fibroblast cells (BJ1). The obtained data indicated that compounds 14b, 17, and 19 induce cytotoxic activity in the breast MCF7, while compounds 6a, 6b, 11 and 14c showed highly potent activity in the colon cancer cell lines.

Coculture of bacterial levans and evaluation of its anti-cancer activity against hepatocellular carcinoma cell lines.

This research represents a novel study to assess how coculture affects levan yield, structure, bioactivities, and molecular weight. Among the 16 honey isolates, four bacterial strains recorded the highest levan yield. The Plackett-Burman design showed that the coculture (M) of isolates G2 and K2 had the maximum levan yield (52 g/L) and the effective factors were sucrose, incubation time, and sugarcane bagasse.

Evaluation of newly copolymers and their montmorillonite nanocomposite as cold flow improver for petroleum lubricating oil.

The great demand on the energy makes the attention toward modifying lubricating oil. This work tends to prepare the following copolymers; octadecylmethacrylate-co-dodecene (CP) and octadecylmethacrylate-co-hexadecene (CP) by free radical solution polymerization using laboratory prepared octadecylmethacrylate monomer with either 1-dodecene or 1-hexadecene. The same monomers also used to prepare their polymers nanocomposite (NP, NP) with 1% of nanomontmorolonite by emulsion polymerization.

Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and insights.

This research study describes the development of new small molecules based on 2,4-thiazolidinedione (2,4-TZD) and their aldose reductase (AR) inhibitory activities. The synthesis of 17 new derivatives of 2,4-TZDs hybrids was feasible by incorporating two known bioactive scaffolds, benzothiazole heterocycle, and nitro phenacyl moiety. The most active hybrid () was found to inhibit AR in a non-competitive manner (0.

Febuxostat attenuates aluminum chloride-induced hepatorenal injury in rats with the impact of Nrf2, Crat, Car3, and MNK-mediated apoptosis.

Aluminum (Al) is a ubiquitous xenobiotic with known toxicity for both humans and animals. Our study was conducted to investigate the protective role of febuxostat (Feb) against aluminum chloride (AlCl3)-induced hepatorenal injury in rats. Hepatorenal injury was induced by oral administration of AlCl3 (40 mg/kg b.

Comparative Study between a Copolymer Based on Oleic Acid and Its Nanohybrid for Improving the Cold Flow Properties of Diesel Fuel.

The as-synthesized copolymer based on the prepared monomers and its nanohybrid were used for improving the cold flow of diesel fuel that has a vital role in meeting energy needs. The copolymer (AE) was created using the prepared monomers, by free radical solution polymerization of the prepared hexadecylmaleamide and octyloleate ester, and the polymer nanohybrid (NH) was created by emulsion polymerization of the same monomers with 1% nano-SiO. The chemical structures of the copolymer and its nanohybrid were proved by Fourier transform infrared spectroscopy (FTIR), H NMR, dynamic light scattering (DLS), and transmission electron microscopy (TEM).

New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and study.

A new series of 2-aminobenzothiazole hybrids linked to thiazolidine-2,4-dione , 1,3,4-thiadiazole aryl urea and cyanothiouracil moieties was synthesised. The in vitro antitumor effect of the new hybrids was assessed against three cancer cell lines, namely, HCT-116, HEPG-2, and MCF-7 using Sorafenib (SOR) as a standard drug. Among the tested compounds, was the most potent showing IC50 of 5.

Viable production of hydrogen and methane from polluted water using eco-friendly plasmonic Pd-TiO nanocomposites.

Solar-to-fuel conversion is a novel clean energy approach that has gained the interest of many researchers. Solar-driven photocatalysts have become essential to providing valuable fuel gases such as methane and hydrogen. Solar energy has emerged as a renewable, abundant energy source that can efficiently drive photochemical reactions through plasmonic photocatalysis.

Design, synthesis, antitumor, and VEGFR-2 inhibition activities of novel 4-anilino-2-vinyl-quinazolines: Molecular modeling studies.

The antitumor activity of newly synthesized 4-anilino-2-vinylquinazolines 8a-r was measured comparable to sorafenib as a standard drug. The 2-vinylquinazolines 8a-r were evaluated for their in vitro antitumor activity. The most active antitumor agents were subjected to in vitro VEGFR-2 inhibition and apoptotic inducing assay.

Genetic variations in the gene affecting growth traits in sheep.

Background And Aim: Sheep productivity in developing countries is crucial, as this animal is an essential source of meat and wool. () plays an important role in the regulation of muscle mass through the regulation of muscle growth, differentiation, and regeneration. The present study sought to investigate genetic variation in the first intron of the gene and the association of variants with growth traits in major sheep breeds in Egypt (Barki, Ossimi, and Rahmani) and Saudi Arabia (Najdi) using polymerase chain reaction (PCR) and sequencing.

Single-nucleotide polymorphisms in gene associated with growth traits in Egyptian sheep.

Aim: The present study was performed to assess the association of single-nucleotide polymorphisms (SNPs) in the fatty acid-binding protein 4 () gene with birth weight (BW), final weight (FW), and average daily gain (ADG) in three Egyptian sheep breeds.

Materials And Methods: Genomic DNA was extracted from the blood samples of 50 male and female individuals representing Ossimi, Rahmani, and Barki sheep breeds. A 407 bp nucleotide (nt) segment from the first intron of was amplified by polymerase chain reaction, sequenced, and analyzed in the different samples.

Synthetic approaches, anticancer potential, HSP90 inhibition, multitarget evaluation, molecular modeling and apoptosis mechanistic study of thioquinazolinone skeleton: Promising antibreast cancer agent.

New series of compounds bearing 2-thioquinazolinone scaffold were designed, synthesized as HSP90 inhibitors. Anti-proliferative activity of the synthesized compounds was evaluated against HCT-116, Hela and MCF-7 cell lines and compound 5k was found to be the most active member of the entire study with IC of 4.47, 7.

Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting.

A new 2-thioquinazolinones series was designed and synthesized as HSP90 inhibitors based on the structure of hit compound VII obtained by virtual screening approach. Their in vitro anti-proliferative activity was evaluated against three human cancer cell lines rich in HSP90 namely; colorectal carcinoma (HCT-116), and cervical carcinoma (Hela), breast carcinoma (MCF-7). Compounds 5a, 5d, 5e and 9h showed a significant broad spectrum anti-proliferative activity against all tested cell lines.

Mitochondrial DNA genetic variations among four horse populations in Egypt.

Horses are one of the early domesticated animals in the world that changed societies and civilizations on a continent-wide scale. Due to the rare information about the genetic characterization of different horse populations in Egypt, this study aimed to identify the genetic biodiversity and relationships between four horse populations reared in Egypt. Genomic DNA was extracted and mtDNA region was amplified using polymerase chain reaction (PCR).

Association between single nucleotide polymorphism in ovine Calpain gene and growth performance in three Egyptian sheep breeds.

The aim of the present study was to assess the association of single nucleotide polymorphisms (SNPs) of Calpain () gene with birth weight (BW), final weight (FW) and average daily gain (ADG) in three Egyptian sheep breeds: Barki, Rahmani and Ossimi. Blood samples were collected from 108 animals representing the three breeds. DNA was isolated using salting out procedure and then the quality and quantity of DNA extracted were measured.

Regulation of expression of sodA and msrA genes of Corynebacterium glutamicum in response to oxidative and radiative stress.

Promoters of genes encoding superoxide dismutase (sodA) and peptide methionine sulfoxide reductase (msrA) from Cory-nebacterium glutamicum were cloned and sequenced. Promoter region analysis of sodA-msrA was unable to identify putative sites of fixed eventual regulators except for possible sites of fixed OxyR and integra-tion host factor. A study of the regulation of these genes was performed using the lacZ gene of Escherichia coli as a reporter placed under the control of sequences downstream of sodA and msrA.

Tianeptine can be effective in men with depression and erectile dysfunction.

Introduction: Erectile dysfunction (ED) and depression are highly prevalent medical disorders affecting men of diverse cultures throughout the world. Tianeptine is a new antidepressant drug with less adverse effects on sexual functions.

Aim: To evaluate the efficacy of tianeptine in the treatment of mild to moderate depression with ED.

Corynebacterium glutamicum superoxide dismutase is a manganese-strict non-cambialistic enzyme in vitro.

Superoxide dismutase (SOD) of Corynebacterium glutamicum was purified and characterized. The enzyme had a native molecular weight of about 80kDa, whereas a monomer with molecular weight of 24kDa was found on SDS-PAGE suggesting it to be homotetramer. The native SOD activity stained gel revealed a unique cytosolic enzyme.

Iron deficiency in two adolescents with conduct, dysthymic and movement disorders.

Enquiry into a marginally subnormal hemogram in two adolescents with complex conduct, dysthymic and movement disorders uncovered a striking iron deficiency and prompted a trial of replacing psychotropic medication with iron therapy. The rationale of iron therapy for behavioural disturbance was examined from the clinical, neurochemical and psychopharmacological points of view. Although further study is required to confirm the therapeutic efficacy and to define the precise nature of iron deficiency in conduct disorder, the weight of the evidence suggests that correcting the nutrient deficit may be an essential step toward a refinement of therapeutic strategies.