64910-48-1

Upstream product

• 102000-73-7 3-bromo-4-nitrobenzonitrile 
• 593-51-1 methylamine hydrochloride 
• 34662-29-8 1-chloro-5-cyano-2-nitrobenzene 
• 74-89-5 methylamine 
• 218632-01-0 3-fluoro-4-nitrobenzonitrile 
• 92241-87-7 3-methoxy-4-nitrobenzamide 
• 67579-92-4 3-methoxy-4-nitrobenzoic acid chloride 
• 5081-36-7 3-methoxy-4-nitrobenzoic acid 
• 177476-75-4 3-methoxy-4-nitrobenzoinitrile 

Downstream Products

• 64910-49-2 4-amino-3-(methylamino)benzonitrile 
• 53484-14-3 3-methyl-3H-benzoimidazole-5-carbonitrile 
• 6595-25-1 1.2-Dimethyl-6-benzimidazol-carbonitril 
• 864274-02-2 1-methyl-1H-1,2,3-benzotriazole-6-carbonitrile 
• 181867-19-6 1-methyl-1H-benzo[d]imidazole-6-carbaldehyde 
• 412309-37-6 2-(4-cyano-phenyl)-3-methyl-3H-benzimidazole-5-carbonitrile 
• 360791-73-7 2-(2-hydroxybiphenyl-3-yl)-3-methyl-3H-benzoimidazole-5-carbonitrile 

Relevant academic research and scientific papers

Cu-Catalyzed C-H Allylation of Benzimidazoles with Allenes

CuH-catalyzed intramolecular cyclization and intermolecular allylation of benzimidazoles with allenes have been described. The reaction proceeded smoothly with the catalytic system of Cu(OAc)2/Xantphos and catalytic amount of (MeO)2MeSiH. This protocol features mild reaction conditions and a good tolerance of substrates bearing electron-withdrawing, electron-donating, or electron-neutral groups. A new catalytic mechanism was proposed for this copper hydride catalytic system.

N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis

We present the design, synthesis and biological activity of novel N-substituted benzimidazole based acrylonitriles as potential tubulin polymerization inhibitors. Their synthesis was achieved using classical linear organic and microwave assisted techniques, starting from aromatic aldehydes and N-substituted-2-cyanomethylbenzimidazoles. All newly prepared compounds were tested for their antiproliferative activity in vitro on eight human cancer cell lines and one reference non-cancerous assay. N,N-dimethylamino substituted acrylonitriles 30 and 41, bearing N-isobutyl and cyano substituents placed on the benzimidazole nuclei, showed strong and selective antiproliferative activity in the submicromolar range of inhibitory concentrations (IC50 0.2–0.6 μM), while being significantly less toxic than reference systems docetaxel and staurosporine, thus promoting them as lead compounds. Mechanism of action studies demonstrated that two most active compounds inhibited tubulin polymerization. Computational analysis confirmed the suitability of the employed benzimidazole-acrylonitrile skeleton for the binding within the colchicine binding site in tubulin, thus rationalizing the observed antitumor activities, and demonstrated that E-isomers are active substances. It also provided structural determinants affecting both the binding position and the matching affinities, identifying the attached NMe2 group as the most dominant in promoting the binding, which allows ligands to optimize favourable cation???π and hydrogen bonding interactions with Lys352.

Synthesis, computational analysis, and antiproliferative activity of novel benzimidazole acrylonitriles as tubulin polymerization inhibitors: Part 2

We used classical linear and microwave-assisted synthesis methods to prepare novel N-substituted, benzimidazole-derived acrylonitriles with antiproliferative activity against several cancer cells in vitro. The most potent systems showed pronounced activit

Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof

Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS

Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, ne

NOVEL CHEMICAL COMPOUNDS

This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.

Development of serine protease inhibitors displaying a multicentered short (<2.3 ?) hydrogen bond binding mode: Inhibitors of urokinase-type plasminogen activator and factor Xa

Novel scaffolds that bind to serine proteases through a unique network of short hydrogen bonds to the catalytic Ser195 have been developed. The resulting potent serine protease inhibitors were designed from lead molecule 2-(2-hydroxyphenyl)1H-benzoimidazo