No abstract

Two new series of coumarin derivatives incorporating thiazoline and thiazolidinone moieties were designed, synthesized, and investigated in vivo for their anti-inflammatory activities using the carrageenan-induced rat paw edema model and in vitro for their inhibitory activities against the human cyclooxygenase (COX)-1 and COX-2 isoforms. Most of the synthesized compounds demonstrated exceptionally high in vivo anti-inflammatory activity and displayed superior GI safety profiles (0-7% ulceration) as compared to indomethacin. All the bioactive compounds showed in vitro high affinity and selectivity toward the COX-2 isoenzyme, compared to the reference celecoxib with IC50 values ranging from 0.31 to 0.78 μM. The ethyl thiosemicarbazone 2b, thiazoline derivatives 3a, 3b, 5b, 6a, and 7f, and the thiazolidinone compounds 8b and 9a showed the highest in vivo and in vitro anti-inflammatory activities with remarkable COX-2 selectivity. Quantitative structure-activity relationship study (QSAR) was done and resulted in a highly predictive power R(2) (0.908). A molecular docking study revealed a relationship between the docking affinity and the biological results.

Breast and cervical cancers are the most common gender-specific cancers affecting women worldwide. In this investigation, we highlighted the synthesis, VEGFR-2 and p38α MAPK inhibitory activity of new series of fluorinated coumarin-based derivatives featuring a variety of bioactive chemical moieties attached or fused to the coumarin nucleus at the 3 and/or 4 position. The bioactive inhibitors were further assessed for their anti-proliferative effect against human MCF-7 breast cancer and HeLa cervical cancer cell lines, respectively. Most of the tested compounds showed potent preferential inhibition effects against human VEGFR-2 and remarkable anticancer activities in the human breast cancer cell line MCF-7. Compounds 29, 24, and 2 displayed the highest inhibitory activity against VEGFR-2 (94% inhibition) and they were the most potent anticancer agents toward MCF-7 cancer cells with IC values of 7.90, 8.28, and 8.30 μg/mL, respectively. Compound 13 inhibited p38α MAPK phosphorylation with a significant reduction in % cell viability against HeLa cancer cells at 10 and 30 µM. Docking experiments carried out on VEGFR-2 and p38 MAPK crystallographic structures revealed that the active compounds bind to the active sites through H-bonds, arene-cation, and hydrophobic π-π interactions. QSAR analysis demonstrated considerable correlation coefficient (R = 0.76969) and root mean square error (RMSE = 0.10446) values. Also, the residual values between the experimental pIC and predicted pIC are very close, indicating the reliability of the established QSAR model.

No abstract

No abstract

Development of new biostrategies for pest control represents a major eco-friendly achievement. The use of micoorganisms represents one of these biostratigies. Bacillus thuringiensis d-endotoxins are recognized safe and economic biological insecticidal proteins. Green nanotechnology is one of the most promisg approches in this field. Our study, demonstrated that B. thuringiensis (4QSTR1) produced cry proteins, which appeared as stained crystals. The Coomassie Brilliant Blue stain allowed a quick and high productivity evaluation of B. thuringiensis (4QSTR1). Synthesized silver nanoparticles by using Fusarium oxysporum (Fo-AgNPs) were used. Also, the protein crystals and endospores of Bacillus thuringiensis were separated. The bioinsecticidal effect of synthesized Fo-AgNPs, Bacillus thuringiensis (Bt) and propolis extracts (ethanolic extract (EEP) and water extract (WEP)) against Tetranychus urticae Koch and Tetranychus cinnabarinus (Boisduval) was evaluated. Bioassays results showed that the insecticidal efficacy (LC 50 and LC 90 ) of Fo-AgNPs were more effective than propolis extracts and Bt against the two species of Tetranychus.

We succeeded in this context to synthesize new fused pyrimidines using ZnO(NPs) as anti-breast cancer agents targeting VEGFR-2 .

No abstract