537677-50-2

Upstream product

• 536974-92-2 (4-(benzyloxy)-3-chloro-5-methoxyphenyl)methanol 
• 62936-23-6 3-chloro-4-hydroxy-5-methoxybenzoic acid 
• 19463-48-0 5-chlorovanillin 
• 37687-67-5 3-chloro-5-(methyloxy)-4-[(phenylmethyl)oxy]benzaldehyde 
• 148869-66-3 4-[N-(1,2,4-triazol-4-yl)amino]benzonitrile 
• 1194-02-1 4-fluorobenzonitrile 
• 536974-93-3 2-benzyloxy-1-chloro-5-chloromethyl-3-methoxybenzene 
• 536974-91-1 4-benzyloxy-3-chloro-5-methoxybenzoic acid benzyl ester 
• 537677-49-9 4-((4-(benzyloxy)-3-chloro-5-methoxybenzyl)(4H-1,2,4-triazol-4-yl)amino)benzonitrile 

Relevant academic research and scientific papers

Synthesis of a new carbon-11-labeled sulfamate derivative as a potential PET tracer for imaging of breast cancer aromatase and steroid sulfatase expression

A carbon-11-labeled sulfamate derivative was designed and synthesized as a new potential positron-emission-tomography dual aromatase-steroid sulfatase inhibitor radiotracer for imaging of aromatase and steroid sulfatase expression in breast cancer. The ta

Dual aromatase-steroid sulfatase inhibitors

By introducting the steroid sulfatase inhibitory pharmacophore into aromatase inhibitor 1 (YM511), two series of single agent dual aromatase-sulfatase inhibitors (DASIs) were generated. The best DASIs in'vitro (JEG-3 cells) are 5, (IC50(aromatase) = 0.82 nM; IC 50(sulfatase) = 39 nM), and 14, (IC50(aromatase) = 0.77 nM; IC50(sulfatase) = 590 nM). X-ray crystallography of 5, and docking studies of selected compounds into an aromatase homology model and the steroid sulfatase crystal structure are presented. Both 5 and 14 inhibit aromatase and sulfatase in PMSG pretreated adult female Wistar rats potently 3 h after a single oral 10 mg/kg dose. Almost complete dual inhibition is observed for 5 but the levels were reduced to 85% (aromatase) and 72% (sulfatase) after 24 h. DASI 5 did not inhibit aldosterone synthesis. The development of a potent and selective DASI should allow the therapeutic potential of dual aromatase-sulfatase inhibition in hormone-dependent breast cancer to be assessed.