Reaction of 6-arylamino-1,3-dialkyluracils with anhydrides of polyfluorocarboxylic acids in the presence of pyridine and subsequent cyclization with concentrated H2SO4 gave the corresponding 1,3-dialkyl-5-(polyfluoroalkyl)pyrimido[4,5-b]quinoline-2,4(1H,3H)-diones (5-polyfluoroalkyl-5-deazaalloxazines). The reactivity of these compounds towards nucleophilic reagents, such as sodium cyanoborohyd...

A series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also show...

Quinaldine (2-methyl quinoline) is a liquid at room temperature, which can be supercooled to reach finally the glassy state. By heating the glass above the glass transition temperature T(g) = 180 K the sample performs two subsequent transitions into, likewise, dielectrically active phases. Thus, the reorientational relaxations of these phases as well as the kinetics of the phase transitions can...

The current assignment depicts the structure of recent quinoline derivatives. This method begins with imine derivatives through condensation reaction ethyl 2-aminobenzoate various substituted aliphatic aldehydes and ketones in existence sodium hydroxide as a catalyst. While second step includes intra-cyclization process compounds presence base like tertiary butoxide that resolute installs hydro...

Asymmetric hydrogenation of quinolines catalyzed by chiral cationic η(6)-arene-N-tosylethylenediamine-Ru(II) complexes have been investigated. A wide range of quinoline derivatives, including 2-alkylquinolines, 2-arylquinolines, and 2-functionalized and 2,3-disubstituted quinoline derivatives, were efficiently hydrogenated to give 1,2,3,4-tetrahydroquinolines with up to >99% ee and full convers...

A highly practical and efficient preparation of pyrano[3,2-c]pyridone and pyrano[3,2-c]quinoline derivatives was developed via an ionic liquid mediated and promoted multi-component reaction of malononitrile, aldehyde, and 4-hydroxyquinolin-2(1H)-one or 4-hydroxy-6-methylpyridin-2(1H)-one. The combinatorial syntheses were achieved for the first time without applying extra activation energy at am...

The reaction  between  trialkyl  phosphites  with  dialkyl  actylenedicarboxylates  in the presence of 2-hydroxyquinoline  (2-quinolinol)  leads  to  β-aminophsphonates derivatives  which  they  have  many applications in medicinal chemistry. When the reaction was performed by triphenylphosphite, a new pyrano quinoline  compounds  were obtained  in  fairly  good  yields. These  compounds also  ...

A highly practical and efficient preparation of pyrano[3,2-c]pyridone and pyrano[3,2-c]quinoline derivatives was developed via an ionic liquid mediated and promoted multi-component reaction of malononitrile, aldehyde, and 4-hydroxyquinolin-2(1H)-one or 4-hydroxy-6-methylpyridin-2(1H)-one. The combinatorial syntheses were achieved for the first time without applying extra activation energy at am...

Two-component reaction of 2-aminobenzophenones with acetylenic esters in the presence of γ-Al2O3 and Cu/ZnO as suitable heterogeneous catalysts has been studied. Nano γ-Al2O3 and Cu/ZnO showed high activities when used as surface catalysts for the synthesis of quinoline derivatives. After completion of the reaction, the catalyst was ...

G-quadruplex (G4)-interactive small molecules have a wide range of potential applications, not only as drugs, but also sensors quadruplex structures. The purpose this work is the synthesis analogues bis-methylquinolinium-pyridine-2,6-dicarboxamide G4 ligand 360A, to identify relevant structure–activity relationships apply design other G4-interactive bearing bis-quinoline or bis-isoquinoline moi...