Glasses have been synthesized in the system P2O5SiO2K2OMgOCaO modified by addition of MoO3. Glasses were prepared by conventional fusion method from 40 g batches. The influence of Mo-cations on the analysed glass structure was investigated by means of Raman and 31P MAS-NMR techniques. It has bee...

Crystals of the molybdenum(III) metaphosphate Mo(PO3)3 were grown by chemical vapor transport with iodine (1173 K → 1073 K). The structure was determined by single crystal X-ray diffraction. Mo(PO3)3 crystallizes in the monoclinic space group Ia , with a = 10.819(1) Å, b = 19.515(3) Å, c = 9.60...

Titin has been purified from rabbit skeletal myofibrils in guanidine hydrochloride by gel filtration on Sephacryl S-1000. The sedimentation coefficients of denatured titin in 6 M guanidine hydrochloride are highly concentration dependent and follow the equation: 1S = 0.241 + 0.302 A280. Equilibr...

2-(5-Methyl-1H-benzimidazol-2-yl)-4-bromo/nitro-phenols (HLBr and HLNO2) and their Zn(II) complexes with ZnX2 (X = Cl, I, NO3) were synthesized and characterized by elemental analysis, molar conductivity, IR, 1H and 13C NMR spectra. The OH proton appears near the NH protons in the 1H NMR spectra...

A novel inhibitor for the adhesion of monocytes to cytokine-stimulated endothelial cells, K-7174, was selected by an assay system using the cultured human monocytic cells and human endothelial cells. K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either ...

K-7174, a GATA-specific inhibitor, is a putative anti-inflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. However, molecular mechanisms involved have not been elucidated. We found that, in glomerular podocytes, induction of monocyte chemoattractant protein...

Preadipocytes constitutively express GATA-2 and GATA-3 that are required to halt the cells at the undifferentiated stage. However, we unexpectedly found that K-7174, a GATA-specific inhibitor, did not induce but rather inhibited differentiation of 3T3-L1 preadipocytes. It was associated with lac...

A liquid chromatography tandem mass spectrometry method was developed and validated for quantification of erlotinib and its metabolites in human plasma. The method is suitable for therapeutic drug monitoring and pharmacokinetic studies.The substances were extracted using protein precipitation, s...

In the screening of six Escherichia coli strains for overexpressing recombinant short-chain dehydrogenases/reductases from Yarrowia lipolytica ACA-DC 50109, an NADPH-dependent carbonyl reductase (YlCR) was identified with capability of producing chiral alcohols. The protein YlCR was over-express...

A series of new 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetamides (6–23) has been synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure tests after intraperitoneal injection in mice. The acute neuro...

Design, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine compounds with promising in vitro (55, 56, 61, 64, 66, and 70–73) and...

Theoretical and experimental studies on the energetics, structure and other physicochemical properties of neutral 1-phenylethanol (1OH), diphenylmethanol (2OH) and triphenylmethanol (3OH) and their corresponding deprotonated anions (oxyanions, formed by deprotonation of the OH group) are reporte...

Flutamide(2-methyl-N-[4-nitro-3-(trifluoromethylphenyl)]propanamide) is a widely used anti-cancer drug. It has been reported that photodermatosis is occasionally induced when an individual taking flutamide is exposed to sunlight. In this study, we found that flutamide undergoes different photore...

The reaction of 2-hydrazino-3-methylquinoxaline 1 with trifluoromethyl-β-diketones 2 not only yields the expected 5-trifluoromethyl-5-hydroxy-Δ2-pyrazolines 3a–3f and/or 3-trifluoromethylpyrazoles 4c–4f but also the unexpected products 1,2,4-triazolo[4,3-a]quinoxalines 5a–5f and/or 3(5)-tri...

The new multicomponent reaction has been found: the pyridine or triethylamine catalyzed multicomponent transformation of salicylaldehydes, 2-aminoprop-1-ene-1,1,3-tricarbonitrile and 3-trifluoromethyl-2-pyrazolin-5-one results in efficient formation of the earlier unknown substituted 2,4-diamino...

α7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the α7 subtype showed metabotropic-like functions, mainly ...

Tripterygium Glycosides (TG) is effective in the treatment of patients with a variety of inflammatory and autoimmune diseases, especially rheumatoid arthritis (RA) in clinical. Wilforlide A (T1) serves as a quality control standard of TG that be listed in Drug Standard of Ministry of Public Heal...

Wilforlide A (WA), an active compound in Tripterygium wilfordii Hook F (TW) which is a traditional Chinese medicine for treatment of autoimmune diseases, is a quality control marker for TW product. At present, the bioavailability/pharmacokinetics of WA is not known. Such information is not only ...

The reaction of 3-amino-4-trifluoromethyl-6-substituted pyrazolo [3,4-b] pyridines (1) with active methylene compounds, such as ethoxy methylene malononitrile, ethyl-(ethoxymethylene)cyanoacetate and 1,3-diketones gave exclusively pyrido [2′,3′:3,4] pyrazolo [1,5-a] pyrimidines (2) and (5), re...

The 4,4-bis(ethoxycarbonyl)-3,4-dihydro-2(1H)-quinolinones 2 were easily synthesized by the oxidative 6-endo-trig cyclization of 2-[2-(N-arylamino)-2-oxoethyl]malonates 1 with manganese(III) acetate in good to excellent yields. The same reaction of N-(2,4-dimethoxyphenyl)-substituted malonate 1t...