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2-Methylquinoxaline reacts with ethyl bromopyruvate giving 2-substituted pyrrolo[1,2-a]quinoxalines. The yield of the condensation depends on the functionalization of starting materials, and optimization is obtained with 2-dimethylamino-3-methylquinoxaline (1c). Reactivity of the resulting pyrrolo[1,2-a]quinoxalines was investigated and supported by a theoretical approach (AM1 calculation performed with the MOPAC 6.0 software). X-ray analysis of 5 which crystallizes in the monoclinic system, space group P21/n, with a = 9.095(1), b = 8.972(1), c = 17.749(3) A, beta = 96.56(1), is also reported.

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Triselenium dicynide (TSD) has been reported for the first time to be a novel cyanation reagent for the microwave-assisted one-pot synthesis of a series of various types of cyano N-heterocycles such as pterin, deazapterin, quinoxaline, naphthyridine, and pyridine in good yields. Copyright Taylor & Francis Group, LLC.

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The quinoxaline scaffold is a promising platform for the discovery of active chemotherapeutic agents. Three series of quinoxaline derivatives were synthesized and biologically evaluated against three tumor cell lines (HCT116 human colon carcinoma, HepG2, liver hepatocellular carcinoma and MCF-7, human breast adenocarcinoma cell line), in addition to VEGFR-2 enzyme inhibition activity. Compounds VIId, VIIIa, VIIIc, VIIIe and XVa exhibited promising activity against the tested cell lines and weak activity against VEGFR-2. Compound VIIIc induced a significant disruption in the cell cycle profile and cell cycle arrest at the G2/M phase boundary. In further assays, the cytotoxic effect of the highly active compounds was determined using a normal Caucasian fibroblast-like fetal lung cell line (WI-38). Compound VIIIc could be considered as a lead compound that merits further optimization and development as an anti-cancer and an apoptotic inducing candidate against the HCT116 cell line.

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It has been shown that alpha-chloroquinoxalines heteroarylate pyridin-2-yl and quinolin-2-ylacetonitriles primarily at the methylene group.A method has been developed for synthesizing 1-R-2-amino-3-heteroarylpyrrolo<2,3-b>quinoxalines permitting the preparation of compounds containing the pyridine and quinoline nuclei.

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The present invention provides a tri-substituted pyrimidine compound having an excellent PDE10 inhibitory activity. The present invention relates to a tri-substituted pyrimidine compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compound for PDE10 inhibitor, and a pharmaceutical composition comprising said compounds as an active ingredient: wherein: either one of X1 and X2 is N, and the other of X1 and X2 is CH; A is *-CH?CH?, *-C(Alk)=CH?, *-CH2?CH2? or *-O?CH2? (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted quinoxalinyl or an optionally substituted quinolyl; Y0 is mono- or di-substituted amino group, or a pharmaceutically acceptable salt thereof.

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A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3- yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, 1H NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.

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A simple method for the introduction of a methyl and higher aliphatic group to various heteroarenes using very inexpensive reagents is described. It is based on the radical addition of a carboxylic xanthate followed by decarboxylation. Depending on the heteroarene structure, the decarboxylation can be spontaneous or induced by heating in N,N-dimethylacetamide or N-methyl pyrrolidone in a microwave oven.

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A simple and efficient procedure for the synthesis of thioglycosides has been achieved from the reaction of glycosylisothiouronium salts with alkyl or heteroaryl halides under microwave irradiation, in much shorter times and in yields comparable with conventional methods. Copyright Taylor & Francis Group, LLC.

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Some complexes of 3d-metals and 2-hydrazinoquinoxalines were synthesized and characterized spectrometrically.These compounds probably exist in solution as tetragonal distorted octahedrons.The organic ligands are to be found at the quadratic base, and anions or solvent-molecules, respectively, at the tops of the octahedron.The existence of chelates can be concluded from i.r. spectra.Together with u.v./vis-spectra back donation can be assumed.An assignment of the u.v./vis-bands is suggested and the ligand-field parameters Dq are estimated.

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The invention discloses a DNA topoisomerase II inhibition activity of modulating kui analogs, its optical isomers, non-enantiomer or a racemic mixture, or its pharmaceutically acceptable salt, solvate, or a prodrug thereof, intermediate or metabolites thereof, the structure of the general formula (I) as shown: Wherein R1 , R2 , R3 , R4 , R5 And Ar in every one of the as defined in this invention. The invention also discloses a process for their preparation, their use as medicament and their application in treating tumors. The compounds of this invention curative effect is precise, small toxic side effect, enriched with the topoisomerase II technology is used for the expression of the drug for the treatment of diseases caused by abnormal inhibitors of types, it is expected to become therapeutic index higher can be used for clinical medicine. (by machine translation)

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