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https://hdl.handle.net/1959.11/20292
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DC Field | Value | Language |
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dc.contributor.author | Moeker, Janina | en |
dc.contributor.author | Teruya, Kanae | en |
dc.contributor.author | Rossit, Sabine | en |
dc.contributor.author | Wilkinson, Brendan | en |
dc.contributor.author | Lopez, Marie | en |
dc.contributor.author | Bornaghi, Laurent F | en |
dc.contributor.author | Innocenti, Alessio | en |
dc.contributor.author | Supuran, Claudiu T | en |
dc.contributor.author | Poulsen, Sally-Ann | en |
dc.date.accessioned | 2017-03-29T15:43:00Z | - |
dc.date.issued | 2012 | - |
dc.identifier.citation | Bioorganic & Medicinal Chemistry, 20(7), p. 2392-2404 | en |
dc.identifier.issn | 1464-3391 | en |
dc.identifier.issn | 0968-0896 | en |
dc.identifier.uri | https://hdl.handle.net/1959.11/20292 | - |
dc.description.abstract | A 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.language | en | en |
dc.publisher | Pergamon Press | en |
dc.relation.ispartof | Bioorganic & Medicinal Chemistry | en |
dc.title | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases | en |
dc.type | Journal Article | en |
dc.identifier.doi | 10.1016/j.bmc.2012.01.052 | en |
dc.subject.keywords | Organic Chemical Synthesis | en |
dc.subject.keywords | Biologically Active Molecules | en |
dc.subject.keywords | Molecular Medicine | en |
local.contributor.firstname | Janina | en |
local.contributor.firstname | Kanae | en |
local.contributor.firstname | Sabine | en |
local.contributor.firstname | Brendan | en |
local.contributor.firstname | Marie | en |
local.contributor.firstname | Laurent F | en |
local.contributor.firstname | Alessio | en |
local.contributor.firstname | Claudiu T | en |
local.contributor.firstname | Sally-Ann | en |
local.subject.for2008 | 030401 Biologically Active Molecules | en |
local.subject.for2008 | 030503 Organic Chemical Synthesis | en |
local.subject.for2008 | 030405 Molecular Medicine | en |
local.subject.seo2008 | 920102 Cancer and Related Disorders | en |
local.subject.seo2008 | 970106 Expanding Knowledge in the Biological Sciences | en |
local.subject.seo2008 | 970103 Expanding Knowledge in the Chemical Sciences | en |
local.profile.school | School of Science and Technology | en |
local.profile.email | bwilkin7@une.edu.au | en |
local.output.category | C1 | en |
local.record.place | au | en |
local.record.institution | University of New England | en |
local.identifier.epublicationsrecord | une-20170323-120337 | en |
local.publisher.place | United Kingdom | en |
local.format.startpage | 2392 | en |
local.format.endpage | 2404 | en |
local.identifier.scopusid | 84858286827 | en |
local.peerreviewed | Yes | en |
local.identifier.volume | 20 | en |
local.identifier.issue | 7 | en |
local.contributor.lastname | Moeker | en |
local.contributor.lastname | Teruya | en |
local.contributor.lastname | Rossit | en |
local.contributor.lastname | Wilkinson | en |
local.contributor.lastname | Lopez | en |
local.contributor.lastname | Bornaghi | en |
local.contributor.lastname | Innocenti | en |
local.contributor.lastname | Supuran | en |
local.contributor.lastname | Poulsen | en |
dc.identifier.staff | une-id:bwilkin7 | en |
local.profile.orcid | 0000-0003-1866-6540 | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.profile.role | author | en |
local.identifier.unepublicationid | une:20490 | en |
dc.identifier.academiclevel | Academic | en |
local.title.maintitle | Design and synthesis of thiourea compounds that inhibit transmembrane anchored carbonic anhydrases | en |
local.output.categorydescription | C1 Refereed Article in a Scholarly Journal | en |
local.search.author | Moeker, Janina | en |
local.search.author | Teruya, Kanae | en |
local.search.author | Rossit, Sabine | en |
local.search.author | Wilkinson, Brendan | en |
local.search.author | Lopez, Marie | en |
local.search.author | Bornaghi, Laurent F | en |
local.search.author | Innocenti, Alessio | en |
local.search.author | Supuran, Claudiu T | en |
local.search.author | Poulsen, Sally-Ann | en |
local.uneassociation | Unknown | en |
local.year.published | 2012 | en |
local.subject.for2020 | 340401 Biologically active molecules | en |
local.subject.for2020 | 340503 Organic chemical synthesis | en |
local.subject.for2020 | 340406 Molecular medicine | en |
local.subject.seo2020 | 280102 Expanding knowledge in the biological sciences | en |
local.subject.seo2020 | 280105 Expanding knowledge in the chemical sciences | en |
Appears in Collections: | Journal Article |
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