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An efficient one-pot synthesis of novel heterocyclic derivatives, 2-aryl-1,4-oxathiino[2,3-b]quinoxalines or -pyrazines 5, via the reaction of 2,3-dichloroquinoxaline or -pyrazine with Na2S×9 H 2O, and subsequent treatment of the resulting 2-chloro-3- sodiosulfanylquinoxaline or -pyrazine 2 with 1-aryl-2-bromo-1-alkanones and then NaH under mild conditions is described. Copyright

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The present invention includes CSNK1A1 inhibitors that are useful in treating or preventing a cancer in a subject. In certain embodiments, the cancer comprises a hematological cancer, such as but not limited to acute myeloid leukemia (AML) and/or MDS (myelodysplastic syndrome, including 5q-MDS). In other embodiments, the cancer comprises colon cancer.

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Focused microwave irradiation of a series of halogenated nitrogen heterocycles and different kinds of nucleophiles in the presence of a catalytic amount of indium trichloride leads to the efficient and completely regioselective generation of aromatic C-C and C-N bonds. The method is simple, rapid, general and inexpensive, and can be performed without the use of dried solvents. Most of the synthetized compounds are new and in many cases the work-up required only filtration. Furthermore, this is the first example of the use of a Lewis acid as a catalyst for heteroarylation, vinylation and amination reactions on pi-deficient heterocyclic substrates.

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Herein, we report the synthesis of different steroidal thiazolo quinoxaline derivatives as antibacterial agents against Escherichia coli. Steroidal ketone thiosemicarbazones (4-6) were obtained from corresponding ketones (1-3) by refluxing with thiosemicarbazide. The thiosemicarbazones on reaction with 2,3-dichloroquinoxalines at 80 C gives 3beta-acetoxy-5alpha-cholestan-6-[thiazolo(4,5-b)quinoxaline-2-yl-hydrazone] (7), 3beta-chloro-cholestan-6-[thiazolo(4,5-b)quinoxaline-2-yl-hydrazone] (8), and 5alpha-cholestan-6-[thiazolo(4,5-b)quinoxaline-2-yl-hydrazone] (9). The structures of the compounds were evident by elemental, IR, 1H NMR and FAB mass spectral analyses. The antibacterial activities of these compounds were evaluated by disk diffusion method against the culture of E. coli and the results were compared with the standard drug amoxicillin. The results reveal that the compounds are better antibacterial agents as compared to amoxicillin. Among all the three compounds (7-9), compound 8 showed better zone of inhibition.

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The partially bridged resortin[4]arene cavitand 1 featuring a cleft-shaped recognition site formed by two anti-quinoxaline bridges and four convergent HO-groups was prepared in three steps and characterised by X-ray crystallography; cavitand 1 was found to be a selective receptor for steroidal substrates in CDCl3, with the best binding observed for steroids with a flat A-ring and two H-bonding sites on rings A and C/D. The Royal Society of Chemistry 2005.

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Compounds of the formula I in which R, R1 and R2 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.

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The invention relates to 2-hydrazone-thiazolo[4,5-b]quinoxaline compounds which are characterized in that the compounds have a general formula represented as the following, wherein R is as the following. The 2-hydrazone-thiazolo[4,5-b]quinoxaline compounds provided by the invention can be used as potential antibacterial and antitumor medicines. The invention also discloses a preparation method thereof.

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The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.

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3-Chloro-6-phenylpyridazine, 2,3-dichloroquinoxaline and 1,4-dichlorophthalazine were reacted with KF under solvent-free conditions in the presence of a phase transfer agent, with or without microwave irradiation. The chlorine-fluorine exchanges were obtained with enhanced yields and selectivities when compared with previous methods.

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In this paper, we introduce a novel and convenient method for the transformation of heterocyclic amides into heteocyclic thioamides. A two-step approach was applied for this transformation: Firstly, we applied a chlorination of the heterocyclic amides to afford the corresponding chloroheterocycles. Secondly, the chloroherocycles and N-cyclohexyl dithiocarbamate cyclohexylammonium salt were heated in chloroform for 12 h at 61C to afford heteocyclic thioamides in excellent yields.

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