374818-89-0

Upstream product

• 96-49-1 [1,3]-dioxolan-2-one 
• 1215-59-4 5-benzyloxy-1H-indole 

Downstream Products

• 714912-31-9 methyl 2-[4-[2-(1-(5-benzyloxy)indolyl)etoxy]phenylthio]isobutyrate 
• 1252592-45-2 4-({2-[5-(benzyloxy)-1H-indol-1-yl]ethyl}(4H-1,2,4-triazol-4-yl)amino)benzonitrile 
• 1252592-46-3 4-{[2-(5-hydroxy-1H-indol-1-yl)ethyl](4H-1,2,4-triazol-4-yl)amino}benzonitrile 
• 1252592-47-4 1-{2-[(4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]ethyl}-1H-indol-5-yl sulfamate 
• 1252592-44-1 2-[5-(benzyloxy)-1H-indol-1-yl]ethyl 4-methylbenzenesulfonate 
• 374818-90-3 N-(2-acetoxyethyl)-5-benzyloxyindole 

Relevant academic research and scientific papers

Bicyclic derivatives of the potent dual aromatase-steroid sulfatase inhibitor 2-bromo-4-{[(4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl} phenylsulfamate: Synthesis, SAR, crystal structure, and in vitro and in vivo activities

The design and synthesis of a series of bicyclic ring containing dual aromatase-sulfatase inhibitors (DASIs) based on the aromatase inhibitor (AI) 4-[(4-bromobenzyl)(4H-1,2,4-triazol-4-yl)amino] benzonitrile are reported. Biological evaluation with JEG-3 cells revealed structure-activity relationships. The X-ray crystal structure of sulfamate 23 was determined, and selected compounds were docked into the aromatase and steroid sulfatase (STS) crystal structures. In the sulfamate-containing series, compounds containing a naphthalene ring are both the most potent AI (39, IC50AROM=0.25 nm) and the best STS inhibitor (31, IC50STS=26 nm). The most promising DASI is 39 (IC50AROM= 0.25 nm, IC50STS=205 nm), and this was evaluated orally in vivo at 10 mgkg-1, showing potent inhibition of aromatase (93%) and STS (93%) after 3 h. Potent aromatase and STS inhibition can thus be achieved with a DASI containing a bicyclic ring system; development of such a DASI could provide an attractive new option for the treatment of hormone-dependent breast cancer.

Neuroprotective and anti-proliferative compounds

This invention features ring-substituted pyrrolo-β-carboline derivatives and ring-substitution and structural derivatives of 3-(1H-indol-3-yl)-1H-pyrrole-2,5-dione of formulas (I-III), which are useful as neuroprotective and anti-proliferative compounds. Also disclosed are methods for the preparation of these compounds, selected biological profiles and uses of these compounds in the treatment of various neurodegenerative and inflammatory diseases of the human nervous system and in the treatment of various other proliferative disorders characterized by loss of growth or cellular differentiation control including, but not limited to, cancer and inflammation.

USE OF α-PHENYLTHIOCARBOXYLIC AND α-PHENYLOXYCARBOXYLIC ACIDS WITH SERUM-GLUCOSE-LOWERING AND SERUM-LIPID-LOWERING ACTIVITY

The use is described of derivatives of α-phenylthiocarboxylic and α-phenyloxycarboxylic acids with formula (I): in which the substituents have the meanings described in the text, for the preparation of a medicine for the prophylaxis and treatment of diabetes, particularly type 2 diabetes, its complications, the various forms of insulin resistance, and hyperlipidaemias.