536974-95-5

Upstream product

• 536974-94-4 [4-(benzyloxy)-3-fluorophenyl]methanol 
• 100-39-0 benzyl bromide 
• 405-05-0 3-fluoro-4-hydroxybenzaldehyde 
• 175968-61-3 3-fluoro-4-[(phenylmethyl)oxy]benzaldehyde 

Downstream Products

• 537677-52-4 4-[(4-benzyloxy-3-fluorobenzyl)[1,2,4]triazol-4-ylamino]benzonitrile 
• 537677-53-5 4-[(3-Fluoro-4-hydroxy-benzyl)-[1,2,4]triazol-4-yl-amino]-benzonitrile 
• 1268821-52-8 5-((4-(benzyloxy)-3-fluoro-benzyl)(4H-1,2,4-triazol-4-yl)amino)biphenyl-2-carbonitrile 
• 1260389-37-4 4-(((6-cyanobiphenyl-3-yl)(4H-1,2,4-triazol-4-yl)amino)methyl)-2-fluorophenyl sulfamate 
• 1260389-55-6 5-((3-fluoro-4-hydroxy-benzyl)(4H-1,2,4-triazol-4-yl)amino)biphenyl-2-carbonitrile 

Relevant academic research and scientific papers

EP300/CREBBP INHIBITOR

The present invention provides a compound having excellent histone acetyltransferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.

AROMATASE INHIBITOR

There is provided a compound of formula (I) wherein Z is selected from N and CR22, wherein R22 is H or a bond with D, wherein D is selected from a bond, C=O, and linear or branched hydrocarbon groups having a carbon chain of from 1 t

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.