Show simple item record

dc.contributor.authorFjellaksel, Richard
dc.contributor.authorBoomgaren, Marc
dc.contributor.authorSundset, Rune
dc.contributor.authorHaraldsen, Ira Hebold
dc.contributor.authorHansen, Jørn H
dc.contributor.authorRiss, Patrick
dc.date.accessioned2020-01-22T09:05:31Z
dc.date.available2020-01-22T09:05:31Z
dc.date.issued2017-08-14
dc.description.abstractIn this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-<i>tert</i>-butylphenyl)-4-piperazinyl-benzimidazole scaffold <i>via</i> Cu-catalysed azide alkyne cycloaddition. Our main purpose was to find a more soluble compound based on the WAY207024 lead with nanomolar potency to inhibit the GnRH receptor. A late stage diversification by the use of click chemistry was, furthermore developed to allow for expansion of the library in future optimisations. All compounds were tested in a functional assay to determine the individual potency of inhibiting stimulation of the receptor by the endogenous agonist GnRH. In conclusion, we found that compound 8a showed improved solubility compared to WAY207024 and nanomolar affinity to GnRH receptor.en_US
dc.identifier.citationFjellaksel R, Boomgaren M, Sundset R, Haraldsen IH, Hansen JHH, Riss P. Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor. MedChemComm. 2017;8(10):1965-1969en_US
dc.identifier.cristinIDFRIDAID 1493769
dc.identifier.doi10.1039/c7md00320j
dc.identifier.issn2040-2503
dc.identifier.issn2040-2511
dc.identifier.urihttps://hdl.handle.net/10037/17162
dc.language.isoengen_US
dc.publisherRoyal Society of Chemistryen_US
dc.relation.journalMedChemComm
dc.relation.projectIDinfo:eu-repo/grantAgreement/RCN/?/?/?/?/?/en_US
dc.rights.accessRightsopenAccessen_US
dc.rights.holderCopyright 2017 The Author(s)en_US
dc.subjectVDP::Mathematics and natural science: 400en_US
dc.subjectVDP::Matematikk og Naturvitenskap: 400en_US
dc.subjectVDP::Medical disciplines: 700::Basic medical, dental and veterinary science disciplines: 710en_US
dc.subjectVDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710en_US
dc.titleSmall molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptoren_US
dc.type.versionpublishedVersionen_US
dc.typeJournal articleen_US
dc.typeTidsskriftartikkelen_US
dc.typePeer revieweden_US


File(s) in this item

Thumbnail

This item appears in the following collection(s)

Show simple item record