31431-19-3Relevant academic research and scientific papers
Preparation method of 3-acetylindole BRPF1 inhibitor and use of 3-acetylindole BRPF1 inhibitor
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, (2020/03/03)
The invention relates to a 3-acetylindole compound of a novel structure shown in a formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate or a solvate thereof, a preparation method of the compound, a pharmaceutical composition containing a therapeutically effective dose of the compound, and use thereof as a protein tyrosine kinase inhibitor, especially as a bromine-containing area PHD zinc finger protein 1 (BRPF1) inhibitor, in the prevention or treatment of disease benefited from the inhibition of BRPF1.
MEBENDAZOLE POLYMORPH FOR TREATMENT AND PREVENTION OF TUMORS
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Sheet 9/17, (2016/09/22)
Mebendazole is an antiparasitic drug with over 40 years of safe use. Recently mebendazole was repurposed for glioblastoma therapy. Three polymorphs of mebendazole exist, but the relative polymorph content for existing drugs varies, and the therapeutic anti-cancer relevance of the different polymorphs was unknown. As an oral drug mebendazole polymorph C is a superior form, and it reaches the brain and brain tumors in effective concentrations. Efficacy is further improved by combining mebendazole with a P-glycoprotein inhibitor. Mebendazole may also be used for therapy of other cancers, as well as a chemo-preventative agent.
Zinc Mediated Friedel-Crafts Acylation in Solvent-Free Conditions under Microwave Irradiation
Paul, Satya,Nanda, Puja,Gupta, Rajive,Loupy, Andre
, p. 2877 - 2881 (2007/10/03)
Zn powder is found to catalyze the Friedel-Crafts acylation of aromatic compounds with acyl halides efficiently under microwave irradiation in solvent-free conditions. Activated substrates undergo acylation predominantly at the para-position. The Zn powder can be re-used up to six times after simple washing with diethyl ether and dilute HCl.
Nitroarylamines via the Vicarious Nucleophilic Substitution of Hydrogen: Amination, Alkylamination, and Arylamination of Nitroarenes with Sulfenamides
Makosza, Mieczyslaw,Bialecki, Maciej
, p. 4878 - 4888 (2007/10/03)
A new reaction of sulfenamides with electrophilic arenes under basic conditions is described. The σ adducts formed from nitroarenes and the anions of sulfenamides undergo elimination of thiol to produce the corresponding o- and/or p-nitroanilines. This reaction is analogous to the known alkylation and hydroxylation of nitroarenes via the vicarious nucleophilic substitution of hydrogen (VNS). The reaction gives access to a wide range of substituted nitroanilines, nitronaphthylamines, and aminoheterocycles. By means of the reaction with N-alkyl- and N-arylsulfenamides, it is possible to obtain N-alkylnitroanilines and nitrodiarylamines. By varying the structure of sulfenamide and the reaction conditions, particularly the nature and concentration of the base, it is possible to control the orientation of animation.
Reactions of Aryl Diazonium Salts and Arylazo Alkyl Ethers. 7. Kinetic Studies of the Decomposition of Z Ethers Derived from Some Substituted 2-Nitrobenzene Diazonium Salts
Broxton, Trevor J.,McLeish, Michael J.
, p. 3673 - 3679 (2007/10/02)
Rate constans for the decomposition of (Z)-syn ethers derived from some 4- or 5-substituted 2-nitrobenzenediazonium salts have been measured in both basic ethanol.For some compounds the rate of decomposition is independent of the base concetration while for others the rate is first order in base concetration.Solvent and substituent effects poit to the base-independent mechanism occuring on the free diazonium salt formed by ionization of the Z ether while the base-dependent mechanism occurs on the Z ether itself.Mechanisms are proposed for each of these reactions.
Antiviral thiazolinyl benzimidazoles
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, (2008/06/13)
Certain thiazolinyl or thiazinyl ketobenzimidazole compounds and derivatives thereof are useful as antiviral agents.
Synthesis and anthelminthic acitivity of alkyl-(5-acyl-1-benzimidazol-2-yl) carbamates
Raeymackers,Van Gelder,Roevens,Janssen
, p. 586 - 594 (2007/10/05)
A series of alkyl-(5-acyl-l-H-benzimidazol-2-yl)-carbamates were prepared and screened for anthelminthic activity. Some of them were found to be fully active at low, atoxic oral dose levels against gastro-intestinal nematodes. The activity against Syphacia muris and Strongyloides ratta is indicated. From these studies methyl (5-benzoyl-1-H-benzimidazol-2-yl) carbamate (mebendazole) and methyl [5-(4-fluorobenzoyl)-1-H-benzimidazol-2-yl]carbamate (flubendazole) were selected for detailed investigation.
Carbonyl-substituted 1-sulfonylbenzimidazoles
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, (2008/06/13)
Certain carbonyl-substituted-1-sulfonylbenzimidazole compounds are useful as antiviral agents.
