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Electric Literature of 49679-45-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 49679-45-0, molcular formula is C11H9ClN2O2, introducing its new discovery.

Quinoxaline chemistry. Part 14. 4-(2-Quinoxalylamino)-phenylacetates and 4-(2-quinoxalylamino)-phenylacetyl-L-glutamates as analogues-homologues of classical antifolate agents. Synthesis and evaluation of in vitro anticancer activity

Among a new series of 26 4-(3-substituted-2-quinoxalylamino)phenylacetates and 4-(3-substituted-2-quinoxalylamino)-phenylacetyl-L-glutamates, eight were selected at NCI for evaluation of their in vitro anticancer activity. The results obtained in comparison with the corresponding nor-compounds series seem to indicate that this type of homologation is not helpful.

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Synthesis of Condensed Quinoxalines. VI. Synthesis of 1H-Pyrazolo<3,4-b>quinoxaline N-Oxides and Related Compounds

Oxidation of 1H-pyrazolo<3,4-b>quinoxalines (1a: R=H, 1b: R=CH3) with m-chloroperbenzoic acid (MCPBA) gave the 4-oxides (2a, b).The structures of 2a, b were confirmed by synthesis, by condensing 2-chloroquinoxaline-3-carbaldehyde 4-oxide (6) with appropriate hydrazines.Further oxidation of 2a with MCPBA gave the 4,9-dioxide (8).Treatment of 1,2-dihydro-2-oxoquinoxaline-3-carboxamide (10) and 1,2-dihydro-2-oxoquinoxaline-3-carbonitrile 4-oxide (13) with a mixture of POCl3 and PCl5 or POCl3-dimethylformamide afforded 2-chloroquinoaline-3-carbonitrile (11) and its 4-oxide (14), respectively.When 11 and 14 were reacted with hydrazines, the correponding 3-amino-1H-pyrazolo<3,4-b>-quinoxalines (12a, b) and their 4-oxides (15a, b) were obtained in high yields.The reaction of ethyl 2-chloroquinoxaline-3-carboxylate (16) with hydrazine hydrate afforded a mixture of uncyclized products, N,N’-bis(2-ethoxycarbonyl-3-quinoxalinyl)hydrazine (17), ethyl 2-hydrazinoquinoxaline-3-carboxylate (18) and 2-hydrazinoquinoxaline-3-carbohydrazide (19).Keywords 1H-pyrazolo<3,4-b>quinoxaline 4-oxide; 1H-pyrazolo<3,4-b>quinoxaline 4,9-dioxide; 3-amino-1H-pyrazolo<3,4-b>quinoxaline 4-oxide; 2-chloroquinoxaline-3-carbaldehyde 4-oxide; hydrazine; N,N’-bis(2-ethoxycarbonyl-3-quinoxalinyl)hydrazine; ethyl 2-hydrazinoquinoxaline-3-carboxylate; 2-hydrazinoquinoxaline-3-carbohydrazide

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Synthesis and pharmacology of some new 2-arylamino-4-oxo<1,3>thiazino<5,6-b>quinoxalines

Several new 2-arylamino-4-oxo<1,3>thiazino<5,6-b>quinoxaline (II) have been synthesized by reacting ethyl 2-chloroquinoxaline-3-carboxylate (I) with various arylthioureas.The compounds possess CNS depressant activity.

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Application of 49679-45-0, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 49679-45-0, molcular formula is C11H9ClN2O2, introducing its new discovery.

Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors

We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogues were synthesized providing useful insight into structure-activity relationships studied. Docking studies realized in the ATP pocket of HsPim-1 are consistent with an unclassical binding mode of these inhibitors. The lead compound 1 was able to block HsPim-1 enzymatic activity at nanomolar concentrations (IC50 of 74 nM), with a good selectivity profile against a panel of mammalian protein kinases. In vitro studies on the human chronic myeloid leukemia cell line KU812 showed an antitumor activity at micromolar concentrations. As a result, compound 1 represents a promising lead for the design of novel anticancer targeted therapies.

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Quinoxaline chemistry. Part 8. 2-[anilino]-3- [carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity

Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared In order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6 M for a few compounds. One single compound exhibited good activity against Candida albicans.

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COMBINATION PHARMACEUTICAL AGENTS AS RSV INHIBITORS

The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.

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Synthesis and Biological Activity of Heterocyclic Derivatives derived from Ethyl-2-hydroxyquinoxaline-3-carboxylate

Ethyl-2-chloroquinoxaline-3-carboxylate obtained from ethyl-2-hydroxyquinoxaline-3-carboxylate upon treatment with morpholine gave ethyl-2-morpholinoquinoxaline-3-carboxylate (1).This ester upon reaction with hydrazine hydrate (99percent) gave respective carboxy hydrazide (2).This hydrazide on reaction with phenyl isothiocyanates gave thiosemicarbazides (3a-c).The thiosemicarbazides on reaction with concentrated sulphuric acid or anhydrous phosphoric acid gave 2-(4-substituted)-anilino-5-((2′-morpholino)quinoxalino)-1,3,4-thiadiazoles (4a-c).The thiosemicarbazides on reaction with 4percent sodium hydroxide formed 4-(para-substituted-phenyl)-3-mercapto-5-((2′-morpholino)quinoxalino)-1,2,4-triazoles (5a-c), and on reaction with I2 in KI gave 2-(4-substituted)anilino-5-((2′-morpholino)quinoxalino)-1,3,4-oxadiazoles (6a-c) respectively.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 49679-45-0, name is Ethyl 3-chloroquinoxaline-2-carboxylate, introducing its new discovery. Safety of Ethyl 3-chloroquinoxaline-2-carboxylate

Quinoxaline chemistry. Part 7. 2-[aminobenzoates]- and 2- [aminobenzoylglutamate]-quinoxalines as classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity

Thirty-three quinoxalines bearing an aminobenxoyl or aminobenzoylglutammate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31.37) the antifungal activity was prevailing.

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Pyrimidine or triazine derivatives and herbicides

A herbicide containing a pyrimidine or triazine derivative of the formula (I): STR1 [wherein A is a furan ring, a pyrimidine ring, a 1,2,4-triazine ring or the like which may suitably be substituted, R is a hydroxyl group or a lower alkoxy group, each of R1 and R2 which may be the same or different, is a halogen atom, a lower alkyl group or a lower alkoxy group, W is an oxygen atom or a sulfur atom, and Z is nitrogen or a methine group] and its salt, as an active ingredient, is presented. The pyrimidine or triazine derivative of the present invention has excellent herbicidal effects against noxious weeds in paddy fields, upland fields and non-agricultural fields.

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Synthesis and evaluation of in?vitro antiproliferative activity of new ethyl 3-(arylethynyl)quinoxaline-2-carboxylate and pyrido[4,3-b]quinoxalin-1(2H)-one derivatives

We report a novel series of quinoxaline derivatives from which agents with antiproliferative activity have been identified. Two ethyl 3-(arylethynyl)quinoxaline-2-carboxylates demonstrated substantial antiproliferative activity against both human non-small cell lung carcinoma (A549) and glioblastoma (U87-MG) cell lines. Pyrido[4,3-b]quinoxalin-1(2H)-ones demonstrated poor activity against A549 and U87-MG cell lines. Three of the derivatives in ethyl 3-(arylethynyl)quinoxaline-2-carboxylate series demonstrated substantial antiproliferative activity. The arylethynyl derivative 2a and 2d proved to be the most cytotoxic with an IC50value of 3.3?muM for both A549 and U87-MG cell lines.

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