18820-83-2Relevant articles and documents
Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit
Gazit, Aviv,Yee, Kevin,Uecker, Andrea,Boehmer, Frank-D.,Sjoeblom, Tobias,Oestman, Arne,Waltenberger, Johannes,Golomb, Gershon,Banai, Shmuel,Heinrich, Michael C.,Levitzki, Alexander
, p. 2007 - 2018 (2003)
Here we report on novel quinoxalines as highly potent and selective inhibitors of the type III receptor tyrosine kinases PDGFR, FLT3, and KIT. These compounds, tricyclic quinoxalines, were generated in order to improve bioavailability over the highly hydrophobic bicyclic quinoxalines. Four of the highly active compounds were characterized in detail and are shown to inhibit PDGFR kinase activity of the isolated receptor as well as in intact cells in the sub-micromolar concentration range. We show that the most active inhibitor (compound 13, AGL 2043) is ~15-20 times more potent than its isomer (compound 14, AGL 2044). We therefore compared the three dimensional structures of the two compounds by X-ray crystallography. These compounds are also highly effective in blocking the kinase activity of FLT3, KIT, and the oncogenic protein Tel-PDGFR in intact cells. These compounds are potent inhibitors of the proliferation of pig heart smooth muscle cells. They fully arrest the growth of these cells and the effect is fully reversible. The chemical, biochemical and cellular properties of these compounds as well as the solubility properties make them suitable for development as anti-restenosis and anti-cancer agents.
Synthesis of a two-dimensional organic-inorganic bismuth iodide metalate through: In situ formation of iminium cations
Dehnhardt, Natalie,Luy, Jan-Niclas,Szabo, Marvin,Wende, Mirco,Tonner, Ralf,Heine, Johanna
, p. 14725 - 14728 (2019)
(Me2CNMe2)Bi2I7 represents a new layered organic-inorganic iodido bismuthate. It displays an unprecedented anion topology, a low band gap and good stability. Advanced electronic structure analysis finds the I?I interactions to be decisive for the compound's structural and electronic properties.
The effect of organic cations on the electronic, optical and luminescence properties of 1D piperidinium, pyridinium, and 3-hydroxypyridinium lead trihalides
Bahnemann, D. W.,Emeline, A. V.,Kevorkyants, R.,Rozhkova, Yu. A.,Selivanov, N. I.
, p. 4390 - 4403 (2020/04/17)
We present a structural and optoelectronic study of 1D piperidinium, pyridinium, and 3-hydroxypyridinium lead trihalides. In contrast to the piperidinium and pyridinium species whose single inorganic chains [PbX31-]n are separated by organic cations, the 3-hydroxypyridinium compound is characterized by double inorganic chains. According to DFT the valence and conduction bands of the piperidinium lead trihalides are composed of occupied p-orbitals of the halogen anions and unoccupied p-orbitals of the Pb2+ cations. In contrast, the pyridinium species feature low-lying cationic energy levels formed from the cation's π?-orbitals. Thus, electronic transitions between the cationic energy levels and valence bands require less energy than valence to conduction band transitions in the case of piperidinium lead trihalides. The presence of an OH group in the pyridinium ring leads to a bathochromic shift of the cationic energy levels resulting in a decreased energy of transitions from the cationic energy levels to the valence band. Electronic transitions predicted by DFT are observable in experimental optical absorption and luminescence spectra. This study paves the way for creation of 1D perovskite-like structures with desired optoelectronic properties.
(HPy)2(Py)CuBi3I12, a low bandgap metal halide photoconductor
Gerhard, Marina,Heine, Johanna,M?bs, Jakob
supporting information, p. 14397 - 14400 (2020/11/07)
Bismuth halides represent an emergent class of materials that combines semiconductor properties with non-toxic constituents. However, many simple bismuth halide compounds feature bandgaps that are significantly higher than those of the lead halide perovskites, which they are supposed to replace. One way to address this issue is the preparation of multinary metal halide materials that feature an additional metal ion. Here, we report on the synthesis and properties of (HPy)2(Py)CuBi3I12 (1) a new copper iodido bismuthate, a photoconductor, which shows a low band gap of 1.59 eV and good thermal and air stability. This journal is
Cyclic amidine hydroiodide for the synthesis of cyclic carbonates and cyclic dithiocarbonates from carbon dioxide or carbon disulfide under mild conditions
Aoyagi, Naoto,Furusho, Yoshio,Endo, Takeshi
supporting information, (2019/12/09)
Hydroiodides of amidines can catalyze the reaction of carbon dioxide and epoxides under mild conditions such as ordinary pressure and ambient temperature, and the corresponding five-membered cyclic carbonates were obtained in high yields. The reaction of epoxide with carbon disulfide was also examined under the same conditions. Detailed investigation showed that the catalytic activity was highly affected by the counter anions of the amidine salts; the iodides were effective catalysts for both of the reaction of epoxide with carbon dioxide and carbon disulfide, whereas the bromide, chloride and fluoride counterparts exhibited almost no catalysis.
Protic onium salts-catalyzed synthesis of 5-aryl-2-oxazolidinones from aziridines and CO2 under mild conditions
Yang, Zhen-Zhen,Li, Yu-Nong,Wei, Yang-Yang,He, Liang-Nian
supporting information; experimental part, p. 2351 - 2353 (2011/10/31)
Protic onium salts, e.g. pyridium iodide, proved to be highly efficient and recyclable catalysts for the selective synthesis of 5-aryl-2-oxazolidinones under a CO2 atmosphere at room temperature, presumably due to aziridine activation assisted by hydrogen bonding on the basis of 1H NMR and in situ FT IR under CO2 pressure study.
Acyl iodides in organic synthesis: XIII.* Reaction of acyl iodides with nitrogen-containing heteroaromatic compounds
Voronkov,Vlasov,Vlasova
experimental part, p. 1838 - 1842 (2011/04/15)
Reactions of acetyl iodide with pyridine at room temperature and with quinoline both at 20-25°C and on cooling to -50°C involve dehydrohalogenation of acetyl iodide with formation of ketene and pyridinium or quinolinium iodides. The reaction of acetyl iodide with pyridine at -5 to -50°C led to the formation of N-acetylpyridinium iodide. Benzoyl iodide reacted with both pyridine and quinoline at both -50°C and at 20-25°C to form stable N-benzoylpyridinium and N-benzoylquinolinium iodides. The reaction of pyrrole with acetyl iodide under analogous conditions was accompanied by polymerization. Pleiades Publishing, Ltd., 2010.
Pyridinium halides and their mixtures as inhibitors of steel corrosion in sulfuric acid solutions
Yurchenko,Ivashchenko,Pilipenko,Pogrebova
, p. 511 - 513 (2008/02/02)
Mixtures of 1-acylmethylpyridinium halides with equimolar amounts of pyridinium halides were prepared by the Ortoleva-King reaction. The inhibiting effect of various pyridinium halides and their mixtures on corrosion of steel in sulfuric acid solutions was studied.
Synthetic routes for a new family of chiral tetradentate ligands containing pyridine rings
Dueggeli, Matias,Goujon-Ginglinger, Catherine,Ducotterd, Sarah Richard,Mauron, David,Bonte, Christophe,Von Zelewsky, Alexander,Stoeckli-Evans, Helen,Neels, Antonia
, p. 1894 - 1899 (2007/10/03)
A series of new tetradentate ligands containing two bipyridine groups or two pyridine moieties carrying amine substituents has been synthesised either from 5′- and 6′-substituted chiral bipyridines, or from chiral pyridine derivatives. These precursors ha
Pyrrolidinone derivatives, their preparation and pharmaceutical composition comprising the same
-
, (2008/06/13)
The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.