Novel tropane analogues as Hsp90 inhibitors targeting colon cancer: Synthesis, biological estimation, and molecular docking study.

New derivatives of tropane scaffold were prepared from the reaction of their thione or thioamide derivatives with α-halocarbonyl compounds. The structures of all new derivatives were assured and proved with their spectral data. The novel tropane derivatives were examined for their cytotoxicity on two colon tumor cell lines; Caco2 and HCT116 cells.

Synthesis and study of pyrimidine-phthalimide hybrids as VEGFR2 inhibitors with antiproliferative activity.

Thalidomide, a once notorious sedative, is now clinically used as an antitumor agent. We aimed to use it as a lead compound for designing pyrimidine-phthalimide hybrids. Nucleophilic substitution reaction of thalidomide analog with primary and/or secondary aliphatic amines afforded pyrimidine-phthalimide hybrids , and .

Conductive polythiophene/graphitic-carbon nitride nanocomposite for the detection of ethanol mixing in petrol.

The automobile vehicles must be operated on fuel containing no more than 10% ethanol. Use of fuel having more than 10% ethanol may cause engine malfunction, starting and running issues, and material degradation. These negative impacts could cause irreversible damage to the vehicles.

Fighting Antibiotic Resistance: New Pyrimidine-Clubbed Benzimidazole Derivatives as Potential DHFR Inhibitors.

The present work describes the design and development of seventeen pyrimidine-clubbed benzimidazole derivatives as potential dihydrofolate reductase (DHFR) inhibitors. These compounds were filtered by using ADMET, drug-likeness characteristics calculations, and molecular docking experiments. Compounds , , , , , , and were chosen for the synthesis based on the results of the in silico screening.

Synthesis of a new series of pyrazolo[1,5-a]pyrimidines as CDK2 inhibitors and anti-leukemia.

Based on the structural study of previously known CDK2 inhibitors, a new series of pyrazolo[1,5-a]pyrimidine derivatives was designed and synthesized. The target compounds were biologically assessed as potent CDK2 inhibitors and promising anti-leukemia hits. The 7-(4-Bromo-phenyl)-3-(3-chloro/2-chloro-phenylazo)-pyrazolo[1,5-a]pyrimidin-2-ylamines 5 h and 5i revealed the best CDK2 inhibitory activity with comparable potency (IC = 22 and 24 nM, respectively) to that of dinaciclib (IC = 18 nM).

Phytoassisted synthesis and characterization of palladium nanoparticles (PdNPs); with enhanced antibacterial, antioxidant and hemolytic activities.

With increasing demand for the treatment of microbial resistance around the globe, it is necessary to develop metallic nanoparticles , ideally by the use of nontoxic medium i.e. plant constituents, that could arrest the microbial growth.

Preparation of multifunctional long-persistent photoluminescence cellulose fibres.

Simple preparation of flame-retardant, photoluminescent, and superhydrophobic smart nanocomposite coating was developed and applied onto cotton fibres using the simple pad-dry-cure technique. This novel strategy involved the immobilization of rare-earth-doped aluminium strontium oxide (ASO; SrAl O :Eu ,Dy ) nanoparticles, environmentally friendly room temperature vulcanizing silicone rubber (RTV) and environmentally friendly Exolet AP422 (Ex). The fabrics were also able to produce a char film in the fire-resistant assessment, providing fibres with a self-extinguishing characteristic.

Novel biologically active polyurea derivatives and its TiO-doped nanocomposites.

A new series of polyurea derivatives and its nanocomposites were synthesised by the solution polycondensation method through the interaction between 4(2-aminothiazol-4-ylbenzylidene)-4-(tert-butyl) cyclohexanone and diisocyanate compound in pyridine. The PU structure was confirmed using Fourier transform-infrared (FTIR) spectroscopy and characterised by solubility, viscometry, gel permeation chromatography (GPC), and X-ray diffraction (XRD) analysis. In addition, PU was evaluated by TGA.