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Triplet quantum yields of five diazanaphthalenes in room temperature solution have been determined.These values indicate that, except in the case of quinoxaline, internal conversion competes as a nonradiative decay mechanism for the excited singlet state.Rates of intersystem crossing and internal conversion in these molecules are determined.Solvent effects on the phthalazine triplet quantum yield are interpreted in terms of perturbations on the states involved.

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1,75-Naphthyridine – Wikipedia,
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A novel light-responsive supramolecular polymer was demonstrated from an overcrowded alkene switch (OAS) mounted with two rigid 2-ureido-4-pyrimidinone (UPy) groups. By strong quadruple hydrogen bonding interactions, transOAS-Upy could form well-defined nanospheres in chloroform, which would be transformed into worm-like assemblies after UV irradiation. Moreover, the inverse process of this system could be achieved by exposure to heat.

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1,177-Naphthyridine – Wikipedia,
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This paper aims to develop a method to impart polyacrylonitrile (PAN) fabric durable flame retadancy. PAN fabric was modified with hydroxylamine hydrochloride (HA) to prepare amidoxime PAN fabric (A-PAN) followed by phosphorylation with phosphoric acid (PA) to obtain flame retardant PAN fabric (P-A-PAN). Thermogravimetric (TG) analysis, differential scanning calorimetry (DSC), microscale combustion calorimetry (MCC) and pyrolysis-gas chromatography-mass spectrometry (Py-GC/MS) were used to analyze the thermal degradation process and flame retardant mechanisms. The structure of the fabrics was characterized by Fourier transform infrared spectroscopy (FTIR) and X-ray Photoelectron Spectroscopy (XPS). The surface morphology of fabrics was observed by scanning electron microscope (SEM). Moreover, the flame retardancy of fabrics before and after washing was evaluated by Limiting oxygen index (LOI) and horizontal burning test. The results showed that the P-A-PAN possessed an excellent thermal stability with the highest LOI value of 34.1% and the highest char residue of 55.67% at 800 C. Most importantly, the P-A-PAN possessed a wonderful flame retardant durability with a little decrease of LOI after 20 washing cycles. When they were ignited, the P-A-PAN fabrics before and after washing were both nonflammable due to the char residue formation of modified fabric.

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1,297-Naphthyridine – Wikipedia,
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This paper presents a new family of pyrimidine-based BF2 complexes. The series contains six examples of 1,1-difluoro-3-aryl(heteroaryl)-1H-pyrimido[1,2-c][1,3,5,2]oxadiazaborinin-9-ium-1-uides (2) ? in which aryl(heteroaryl) = phenyl, 4-MeC6H4, 4-N(CH3)2C6H4, 4-NO2C6H4, 2-naphthyl, and 2-thienyl. The heterocycles 2 were easily synthesized at yields of 50?68% from reactions ? at room temperature for 24 h ? of simple N-(pyrimidin-2-yl)benzamides (1) with BF3¡¤Et2O, and they were fully characterized by 1H-, 13C-, 19F, 11B-NMR, GC?MS, and X-ray diffractometry. Moreover, the photophysical properties, TD-DFT analysis, BSA-binding experiments, and molecular docking studies for the new organoboron complexes 2 were determined, presented, discussed, and compared with similar compounds that have already been described.

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1,76-Naphthyridine – Wikipedia,
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Combinations of antiretroviral drugs are successfully used to treat HIV-infected patients. However, drug resistance is a major problem that makes discovery of new antiretroviral drugs an ongoing priority. The ribonuclease H (RNase H) activity of the HIV-1 reverse transcriptase catalyzes the selective hydrolysis of the RNA strand of RNA:DNA heteroduplex replication intermediates, and represents an attractive unexploited target for drug development. This review reports on recent progress in the characterization of HIV-1 RNase H inhibitors from 2013 to 2016, describing their chemical structures, structureactivity relationship and binding modes. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of RNase H inhibitors.

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Metal-free reaction between quinolines, aryltrifluoroacetylacetylenes and water at -18 C-rt in MeCN resulted in stereoselective assembly of trifluoromethylated oxazinoquinolines with up to 99% yield that was essentially in contrast to a similar reaction with pyridines. The annulation proceeded via the 1,3-dipolar adducts of quinolines with trifluoroacetylacetylenes followed by intramolecular cyclization involving the trifluoroacetyl group and a molecule of water.

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1,266-Naphthyridine – Wikipedia,
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Signaling through the fibroblast growth factor receptor (FGFR) tyrosine kinase is crucial to a number of key pharmacological processes; however, dysregulation of this signaling is observed with a number of different cancers suggesting that inhibition of FGFR may provide an important therapeutic agent in the treatment of cancers. This chapter provides an overview of the development of FGFR inhibitors beginning with the identification of nonselective FGFR inhibitors, then describing the medicinal chemistry optimization resulting in the delivery of a number of highly selective FGFR inhibitors, some of which are currently being assessed in clinical trials. The development of isoform selective FGFR inhibitors as well as covalent inhibitors and inhibitors of the inactive form of FGFR are also described.

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1,224-Naphthyridine – Wikipedia,
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The tetracationic complex [Rh2(MeCN)2(Naft)4](BF4)4 (Naft = mu-1,8-naphthyridine) was found to be an efficient catalyst for the silylformylation of internal and functionalised alkynes to yield useful synthetic intermediates. The complex exhibits an unprecedented chemoselectivity towards alkyne silylformylation instead of simple hydrosilylation, as well as a good stereoselectivity. The catalytic efficiency of the complex is markedly superior compared to that of previously reported catalysts such as [Rh+ C7 H8 BPh4-] or Rh4(CO)12; incidentally, the performance of the latter catalyst was found to vary dramatically with its shelf-life, which indicates that the catalyst evolves with ageing towards other species, most notably higher nuclearity rhodium carbonyl clusters, which are more chemoselective towards silylformylation. Preliminary results on the determination of the catalytically active species in the case of complex [Rh2(MeCN)2(Naft)4](BF4)4 indicate that the complex is reduced in situ to a dirhodium(I) species which maintains the dimeric, lantern-shaped structure.

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1,68-Naphthyridine – Wikipedia,
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The synthesis of cationic dirhodium(II) complexes by partial or total substitution of the acetate groups of [Rh2(OAc)4] with different homoleptic neutral bidentate ligands has been attempted. The ligand 1,8-naphthyridine gave the best results: substitution of one as well as of all four acetate ligands is possible, giving rise to mono-, di- and tetra-cationic complexes. One of the resulting tetrasubstituted complexes has been structurally characterised and found to exhibit the expected lantern-shaped structure. All cationic complexes have been investigated as catalysts in different reactions involving silanes: promising results have been obtained, particularly in the silylformylation of alkynes.

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O’NEIL, Jennifer; BENITA, Yair; MARINE, Shane; HAINES, Brian

The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an ¡Àv23 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof.

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