Please use this identifier to cite or link to this item: https://hdl.handle.net/1959.11/20292
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dc.contributor.authorMoeker, Janinaen
dc.contributor.authorTeruya, Kanaeen
dc.contributor.authorRossit, Sabineen
dc.contributor.authorWilkinson, Brendanen
dc.contributor.authorLopez, Marieen
dc.contributor.authorBornaghi, Laurent Fen
dc.contributor.authorInnocenti, Alessioen
dc.contributor.authorSupuran, Claudiu Ten
dc.contributor.authorPoulsen, Sally-Annen
dc.date.accessioned2017-03-29T15:43:00Z
dc.date.issued2012en
dc.identifier.citationBioorganic & Medicinal Chemistry, 20(7), p. 2392-2404en
dc.identifier.issn0968-0896en
dc.identifier.issn1464-3391en
dc.identifier.urihttps://hdl.handle.net/1959.11/20292en
dc.description.abstractA library of 32 novel glycoconjugate thiourea-bridged benzene sulfonamides have been synthesized from the reaction of glycosyl isothiocyanates with a panel of simple benzene sulfonamides comprising either a free amine or hydrazide. All compounds were investigated for their ability to inhibit the enzymatic activity of five human carbonic anhydrase (hCA) isozymes: hCA I, II and membrane-associated isozymes IX, XII and XIV. A physicochemical feature of the free sugar thioureido glycoconjugates was high water solubility (>20 mg/mL), as well many of these compounds exhibited a desirable potency and CA isozyme selectivity profile. From this library several inhibitors displayed excellent potency-selectivity profiles for transmembrane anchored CAs over off-target CA I and II. These molecules provide potential dual-acting candidates for the development of inhibitors that target the extracellular CAs (IX, XII and XIV)-either directly as free sugars (membrane impermeable) or indirectly as acetylated prodrugs, becoming free sugars upon esterase hydrolysis.en
dc.languageenen
dc.publisherPergamon Pressen
dc.relation.ispartofBioorganic & Medicinal Chemistryen
dc.titleDesign and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrasesen
dc.typeJournal Articleen
dc.identifier.doi10.1016/j.bmc.2012.01.052en
dc.subject.keywordsOrganic Chemical Synthesisen
dc.subject.keywordsBiologically Active Moleculesen
dc.subject.keywordsMolecular Medicineen
local.contributor.firstnameJaninaen
local.contributor.firstnameKanaeen
local.contributor.firstnameSabineen
local.contributor.firstnameBrendanen
local.contributor.firstnameMarieen
local.contributor.firstnameLaurent Fen
local.contributor.firstnameAlessioen
local.contributor.firstnameClaudiu Ten
local.contributor.firstnameSally-Annen
local.subject.for2008030401 Biologically Active Moleculesen
local.subject.for2008030503 Organic Chemical Synthesisen
local.subject.for2008030405 Molecular Medicineen
local.subject.seo2008920102 Cancer and Related Disordersen
local.subject.seo2008970106 Expanding Knowledge in the Biological Sciencesen
local.subject.seo2008970103 Expanding Knowledge in the Chemical Sciencesen
local.profile.schoolSchool of Science and Technologyen
local.profile.emailbwilkin7@une.edu.auen
local.output.categoryC1en
local.record.placeauen
local.record.institutionUniversity of New Englanden
local.identifier.epublicationsrecordune-20170323-120337en
local.publisher.placeUnited Kingdomen
local.format.startpage2392en
local.format.endpage2404en
local.peerreviewedYesen
local.identifier.volume20en
local.identifier.issue7en
local.contributor.lastnameMoekeren
local.contributor.lastnameTeruyaen
local.contributor.lastnameRossiten
local.contributor.lastnameWilkinsonen
local.contributor.lastnameLopezen
local.contributor.lastnameBornaghien
local.contributor.lastnameInnocentien
local.contributor.lastnameSupuranen
local.contributor.lastnamePoulsenen
dc.identifier.staffune-id:bwilkin7en
local.profile.orcid0000-0003-1866-6540en
local.profile.roleauthoren
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local.identifier.unepublicationidune:20490en
dc.identifier.academiclevelAcademicen
local.title.maintitleDesign and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrasesen
local.output.categorydescriptionC1 Refereed Article in a Scholarly Journalen
local.description.statisticsepubsVisitors: 20<br />Views: 135<br />Downloads: 0en
local.search.authorMoeker, Janinaen
local.search.authorTeruya, Kanaeen
local.search.authorRossit, Sabineen
local.search.authorWilkinson, Brendanen
local.search.authorLopez, Marieen
local.search.authorBornaghi, Laurent Fen
local.search.authorInnocenti, Alessioen
local.search.authorSupuran, Claudiu Ten
local.search.authorPoulsen, Sally-Annen
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