1039987-39-7

Upstream product

• 585-71-7 (1-bromoethyl)benzne 
• 95-54-5 1,2-diamino-benzene 
• 98-86-2 acetophenone 
• 13534-98-0 3-bromopyridin-4-amine 
• 618-36-0 rac-methylbenzylamine 
• 31488-84-3 2-nitro-N-(1-phenylethyl)aniline 
• 1493-27-2 ortho-nitrofluorobenzene 
• 34801-09-7 N-(2-aminophenyl)acetamide 

Downstream Products

• 1172627-51-8 3-(4-chlorophenyl)-1-(1-phenylethyl)-1,4-dihydroquinoxaline 
• 380551-61-1 [1-(1-phenylethyl)-1H-benzimidazol-2-yl]methanol 

Relevant academic research and scientific papers

General synthesis of 1-substituted 2-methylbenzimidazoles from ketones and 2-aminoacetanilide

A novel method for preparation of 1-substituted benzimidazoles via reductive amination of ketones with N-differentiated 1,2-diaminobenzenes is described. The method appears to be general in application to acyclic and cyclic ketones, as well as heteroatom-

Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy

As epigenetic readers, bromodomain and extra-terminal domain (BET) family proteins bind to acetylated-lysine residues in histones and recruit protein complexes to promote transcription initiation and elongation. Inhibition of BET bromodomains by small molecule inhibitors has emerged as a promising therapeutic strategy for cancer. Herein, we describe our efforts toward the discovery of a novel series of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as BET inhibitors. Intensive structural modifications led to the identification of compound 35f as the most active inhibitor of BET BRD4 with selectivity against BET family proteins. Further biological studies revealed that compound 35f can arrest the cell cycle in G0/G1 phase and induce apoptosis via decreasing the expression of c-Myc and other proteins related to cell cycle and apoptosis. More importantly, compound 35f showed favorable pharmacokinetic properties and antitumor efficacy in MV4-11 mouse xenograft model with acceptable tolerability. These results indicated that BET inhibitors could be potentially used to treat hematologic malignancies and some solid tumors.

Rapid construction of imidazopyridines from ortho-haloaminopyridines

A practical strategy for the preparation of imidazopyridine derivatives from ortho-haloaminopyridines utilizing a two-step C-N coupling/cyclization reaction sequence has been developed. This procedure provides rapid and efficient access to many medicinally interesting imidazopyridine compounds and related imidazopyrazine/purine heterocycles.

TNF -Alpha Modulating Benzimidazoles

A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.