The multistep synthesis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one 15 has been carried out. The compound showed antiproliferative and apoptotic effects against K562, K562-R (imatinib mesilate resistant), HL60 and multidrug resistant (MDR)...
Ethyl 3,5-dimethyl-4-[3-(2-nitro-phenyl)-acryloyl]-1H-pyrrole-2-carboxylate (EDNPAPC) has been synthesized and characterized by 1H NMR, UV–Vis, FT-IR and Mass spectroscopy. Geometrical, spectral, thermodynamic properties have been calculated and evaluated using DFT level of theory, B3LYP functi...
A new series of some novel isoniazid condensed 1,4-dihydropyridines was prepared by reaction of N-(3-oxobutanoyl) isonicotinohydrazide with aryl aldehyde and 25–30% ammonia solution in the presence of catalytic amount of barium nitrate as an efficient catalyst. The confirmation of the chemical ...
The standard (po = 0.1 MPa) molar enthalpies of combustion in oxygen, at T = 298.15 K, for crystalline 3,5-dimethylpyrazole (Me2Pyr), 3,5-dimethyl-4-nitrosopyrazole (Me2PyrNO), 1,3,5-trimethyl-4-nitrosopyrazole (Me3PyrNO), and 3,5-dimethyl-1-phenyl-4-nitrosopyrazole (Me2PhPyrNO) were measured ...
A simple and efficient methodology was developed for the synthesis of new 4-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylazo)-N-(2-substituted-4-oxo-4H-quinazolin-3-yl)benzenesulfonamide derivatives 10a–10j in good amount of yields. They have been prepared using 2-acetamidobenzoic acid derivatives 2a–...
Several-1-carbothioamide-3,5-dimethyl-4-[(substituted phenyl) diazenyl] pyrazoles 2a–d, 1-(pyridine-4-ylcarbonyl)-3,5-dimethyl-4-[(substituted phenyl) diazenyl] pyrazoles 3a–d, 1-(5-chloro-6-fluoro-1,3-benzothiazole-2-yl)thiocarbamoyl-3,5-dimethyl-4-[(substituted phenyl) diazenyl] pyrazoles 4a...
We perform a theoretical investigation about the excited state intramolecular proton transfer (ESIPT) reaction for a novel 2-(2-hydroxy-3,5-dimethyl-phenyl)-benzooxazole-5-carboxylicacid (HDPBC) system. The ultrafast excited state process is due to the low potential barrier, which should be the ...
Halenaquinol sulfate, a hydroquinone sulfate obtained from the sponge Xestospongia sapra, prevented cell membrane fusion events of echinaderm gametes but did not affect early embryonic development of fertilized eggs up to the gastrula stage. However, halenaquinol sulfate inhibited secretion of h...
Two hexaprenylhydroquinone derived disulfates, shaagrockol B and C (1 and 2) were isolated from the Red Sea sponge Toxiclona toxius (Levi, 1958). The structure of these two new hexaprenoid, antifungal metabolites was determined by spectroscopic methods, mainly 2D-NMR measurements as well as chem...
High acid crudes contain large amounts of naphthenic acids (NAs), which lead to severe corrosion in oil refinery equipment and serious environmental problems. The goal of this study is to develop a non-catalytic supercritical methanol (scMeOH) route for effective deacidification of NA mixtures a...
Unexpected inhibitory effects against eeAChE could be found for a newly synthesized class of caffeic acid phenethyl ester (CAPE) derivatives. Thus, phenethyl-(E)-3-(3,5-dimethoxy-4-phenethoxyphenyl)-acrylate (Ki = 1.97 ± 0.38 μM, Ki´ = 2.44 ± 0.07 μM) and 4-(2-(((E)-3-(3,4-bis(benzyloxy)phe...
By combining the scaffolds of UI-125 and Sorafenib, a series of bis-aryl ureas and amides based on 2-amino-3-purinylpyridine moiety were designed and synthesized as novel DFG-out B-RafV600E inhibitors. Among them, 20c–e, 20g and 21h displayed potent antiproliferative activities against melanoma...
A variety of novel 2-methylquinazolin-4(3H)-one derivatives (1–29) bearing urea, thiourea and sulphonamide functionalities at position 3 of biological interest have been synthesized and screened for their anti-inflammatory (TNF-α and IL-6) and antimicrobial activities (antibacterial and antifu...
A series of commercially useful substituted pyridyl ureas have been synthesized via selenium dioxide-catalyzed reductive carbonylation of substituted nitrobenzene or substituted nitropyridine with amine as co-reagent and carbon monoxide as carbonyl reagent instead of phosgene in one-pot reaction...
The condensation of 3-cyano-7-diethylamino-iminocoumarin with various isocyanates and diisocyanates as C-electrophiles gave a new series of N-substituted iminocoumarins and bis-iminocoumarins. The ten compounds obtained were characterized using IR, 1H NMR, 13C NMR, elemental analysis and mass sp...
A method for the synthesis and isolation of 1,1′-methylene-bis-(3-aryl-imidazol-2-ylidene) ligands, aryl = 2,6-diisopropyl-phenyl (DiPP), LDiPP, mesityl (mes), Lmes, is reported, which provides synthetically useful quantities of high purity. Derivatisation of LDiPP with chalcogenides gave the a...
Sulfatide induces leukocyte activation, which is thought to be mediated via L-selectin. Here we demonstrate that lymphocytes express a receptor for sulfatide distinct from L-selectin and that this receptor is involved in sulfatide-induced cell activation. While cell surface L-selectin expression...
Publisher SummaryCell surface glycoconjugates have been extensively studied as potential receptors for cell–cell and cell–ligand interactions. Carbohydrates occur on cell surface glycoproteins, glycolipids, and proteoglycans. As glycolipids containing a single oligosaccharide are readily purif...
An immunostaining procedure has been developed for the assay of the gangliotetraose gangliosides and sulfatide in cerebrospinal fluid. Gangliosides of the gangliotetraose series were individually determined with cholera toxin B-subunit (CT-B) and an anti CT-B monoclonal antibody after chromatogr...
Sulfatides (galactosyl ceramide-I3-sulfate) and other sulfated glycolipids are found in many tissues. The cell adhesion proteins laminin, thrombospondin, and von Willebrand factor bind specifically to sulfated glycolipids. Methods for characterizing the specificity of these interactions using su...
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