Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)

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Title

Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)

Content partner

The University of Auckland Library

Collection

ResearchSpace@Auckland

Description

Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers. A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalysed coupling of substituted phenyl or pyridyl bromides with the known morpholino(piperazin-1-yl)methanone, and shown to be potent (IC50∼100nM) and very isoform-selective inhibitors of AKR1C3. Lipophilic electron-withdrawing substituents on the phenyl ring were pos...

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Format

Research paper

Research format

Journal article

Date created

2014-02-01

Creator

Flanagan, Jack / Atwell, GJ / Heinrich, DM / Brooke, DG / Silva, S / Rigoreau, LJM / Trivier, E / Turnbull, AP / Raynham, T / Jamieson, Stephen / Denny, William

URL

http://hdl.handle.net/2292/34204

Related subjects

AKR / Aldo–keto reductase / COX / Computer aided drug design / Crystal structure / DCM / DIPEA / DMSO / Inhibitor / Morpholylureas / NADPH / NSAID / PBD / Protein Data Bank / TFA / aldo–keto reductase / cyclo-oxygenase / dichloromethane / diisopropylethylamine / dimethyl sulfoxide / nicotinamide adenine dinucleotide phosphate / non-steroidal anti-inflammatory drugs / trifluoroacetic acid / 3-Hydroxysteroid Dehydrogenases / Catalytic Domain / Chemistry Techniques, Synthetic / Crystallography, X-Ray / Enzyme Inhibitors / Hydrogen Bonding / Hydroxyprostaglandin Dehydrogenases / Inhibitory Concentration 50 / Models, Molecular / Molecular Structure / Morpholines / Structure-Activity Relationship

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