889472-34-8

Upstream product

• 58881-45-1 Indole-2-carbonyl chloride 
• 100-39-0 benzyl bromide 
• 3770-50-1 2-carbethoxyindole 
• 6921-34-2 benzylmagnesium chloride 

Downstream Products

• 889472-36-0 1-(1H-indol-2-yl)-2-phenylethanone oxime 
• 1173768-22-3 1-(3-{1-(4-methylphenyl)-2-phenyl-3-[3-(trifluoromethyl)phenyl]prop-2-ynyl}-1H-indol-2-yl)ethanone 
• 1173768-25-6 2-phenyl 1-[3-(3-phenyl-1-thien-2-ylprop-2-ynyl)-1H-indol-2-yl]ethanone 

Relevant academic research and scientific papers

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors

Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC50 values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results.

Benzimidazole, benzoxazole and benzothiazole derivatives as 5HT 2B receptor ligands. Synthesis and preliminary pharmacological evaluation

2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2- phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2c subtypes. All compounds were characterized by binding affinity determination for 5-HT 2A and 5-HT2c subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2c subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations. Birkhaeuser Boston 2005.