23876-39-3Relevant articles and documents
Synthesis and antiprotozoal evaluation of benzothiazolopyrroloquinoxalinones, analogues of kuanoniamine A
Tapia, Ricardo A.,Prieto, Yolanda,Pautet, Felix,Walchshofer, Nadia,Fillion, Houda,Fenet, Bernard,Sarciron, Marie-Elizabeth
, p. 3407 - 3412 (2003)
Boc-aminoethylindoloquinone 8, a key intermediate for the building of pentacyclic quinoneimines, analogues of kuanoniamine A, was synthesized by alkylation of 4,7-dimethoxyindole 3 with 1,2-dibromoethane followed by transformation into azide, reduction of the latter with trimethylphosphine in the presence of 2-(tert-butoxycarbonyloximino)-2-phenylacetonitrile and oxydative demethylation of the Boc-amine 6 with silver(II) oxide. Quinone 8 was then treated in situ with the thiazole o-quinodimethane 10 to afford a regioisomeric mixture of the tetracyclic quinones 11. Treatment of the mixture with trifluoroacetic acid and molecular sieves 4-A provided the corresponding quinoneimines 12. Separation of the regioisomers was performed by preparative thin-layer chromatography on silica gel. The structural assignment was made by 2D 1H-13C HMBC correlations performed on the less polar regioisomer 12b. In vitro anti-leishmanial assays showed that the tested compounds possess a good potency towards two Leishmania sp. as well as against a virulent strain of Toxoplasma gondii and without any cytotoxicity against THP-1 cells.
Novel indole derivative and medicine containing the same (by machine translation)
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Paragraph 0152; 0157, (2018/06/30)
[A] formation of Amyloid fibrils can be compounds, including therapeutic or prophylactic agent for neurodegenerative disease Amyloid fibrils formation inhibitor compound and of. (I) or its pharmaceutically acceptable compound represented by the formula [a] or a salt or solvate thereof includes the, Amyloid fibrils formation inhibitor. [R1 And R2 Each independently is H, an alkyl group, a cyano group or the like; R3 And R4 Each independently is H, or an alkyl group; R3 And R4 The, joint may form a ring; Ar1 And Ar2 The substituted or unsubstituted heteroaryl group are independently substituted/unsubstituted aryl groups /; X and Y are each independently a single bond, - (=O) - C etc., Z is O or CH2 ; N is an integer of 1 - 3][Drawing] no (by machine translation)
Synthesis and cytotoxic activity of 2-acyl-1H-indole-4,7-diones on human cancer cell lines
Mahboobi, Siavosh,Sellmer, Andreas,Eichhorn, Emerich,Beckers, Thomas,Fiebig, Heinz-Herbert,Kelter, Gerhard
, p. 85 - 92 (2007/10/03)
Synthesis and cytotoxic activity of a series of 2-acyl-1H-indole-4,7-diones on human cancer cell lines are described. Due to close structural relationship to 2-acylindoles, potent inhibitors of tubulin polymerization, the mode of action of these novel com
Ruthenium-catalyzed heteroannulation of anilines with alkanolammonium chlorides leading to indoles
Cho, Chan Sik,Kim, Jin Hwang,Kim, Tae-Jeong,Shim, Sang Chul
, p. 3321 - 3329 (2007/10/03)
Anilines react with alkanolammonium chlorides in an aqueous medium (H2O-dioxane) at 180°C in the presence of a catalytic amount of a ruthenium catalyst together with SnCl2·2H2O to afford the corresponding indoles in moderate to good yields. Especially, when triisopropanolammonium chloride is employed to react with anilines, 2-methylindoles are formed regioselectively. The presence of SnCl2·2H2O is necessary for the effective formation of indoles. A reaction pathway involving alkanol group transfer from alkanolamines to anilines, N-alkylation of anilines by anilinoalkanols and heteroannulation of 1,2-dianilinoalkanes is proposed for this catalytic process.
Synthesis of novel pentacyclic pyrrolothiazolobenzoquinolinones, analogs of natural marine alkaloids
Bénéteau, Valérie,Besson, Thierry
, p. 2673 - 2676 (2007/10/03)
Multistep synthesis (12 steps) of new pentacyclic compounds, which are structurally very close to natural marine alkaloids, was performed via a Diels-Alder reaction between 4-methylene-5-(bromomethylene)-4,5-dihydrothiazole and a protected dioxotryptamine
Ruthenium-catalyzed synthesis of indoles from anilines and trialkanolammonium chlorides in an aqueous medium
Cho, Chan Sik,Kim, Jin Hwang,Shim, Sang Chul
, p. 1811 - 1814 (2007/10/03)
Anilines react with trialkanolammonium chlorides in an aqueous medium (H2O-dioxane) at 180°C in the presence of a catalytic amount of ruthenium(III) chloride hydrate and triphenylphosphine together with tin(II) chloride dihydrate to afford the corresponding indoles in good yields. (C) 2000 Elsevier Science Ltd.
Synthesis and cytotoxicity of analogues of the antibiotic BE 10988 inhibitors of DNA topoisomerase II
Catrycke, Marc-Olivier,Houssin, Raymond,Henichart, Jean-Pierre,Pfeiffer, Bruno,Renard, Pierre,Dassonneville, Laurent,Bailly, Christian
, p. 2025 - 2030 (2007/10/03)
Indolequinone derivatives of the antitumour antibiotic BE 10988 were synthesized and evaluated for their cytotoxicity and action mechanism. The quinone system is essential to biological activity and the thiazole ring plays a major role in the poisoning of
Ruthenium-catalysed synthesis of indoles from anilines and trialkanolamines in the presence of tin(II) chloride dihydrate
Cho, Chan Sik,Lim, Hyo Kyun,Shim, Sang Chul,Kim, Tae Jeong,Choi, Heung-Jin
, p. 995 - 996 (2007/10/03)
Anilines react with trialkanolamines in dioxane in the presence of a catalytic amount of a ruthenium catalyst together with tin(II) chloride dihydrate to give the corresponding indoles in moderate to good yields.
GENERAL SYNTHESIS OF 2,3-SUBSTITUTED 5-MEMBERED HETEROCYCLIC QUINONES
Cherif, Mahmoud,Cotelle, Philippe,Catteau, Jean-Pierre
, p. 1749 - 1758 (2007/10/02)
4,7-dimethoxybenzofuran, -thiophene, -selenophene and 4,7-dimethoxyindole have been prepared by a two-step procedure involving a cyclization-dehydration of the acetals (1).The oxidative demethylation of 4,7-dimethoxybenzothiophene, -selenophene and