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Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms.

dc.contributor.authorD'ASCENZIO, M
dc.contributor.authorGUGLIELMI, P
dc.contributor.authorCARRADORI, S
dc.contributor.authorSECCI, D
dc.contributor.authorFLORIO, R
dc.contributor.authorMOLLICA, A
dc.contributor.authorCERUSO, M
dc.contributor.authorAkdemir, ATİLLA
dc.contributor.authorSOBOLEV, AP
dc.contributor.authorSUPURAN, CT
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T21:51:28Z
dc.date.available2019-10-05T21:51:28Z
dc.date.issued2017-12-01
dc.description.abstractA large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). They were obtained by reductive ring opening of the newly synthesized N-alkylated saccharin derivatives and were shown to be inactive against the two cytosolic off-target hCA I and II (Kis > 10 µM). Interestingly, these compounds inhibited hCA IX in the low nanomolar range with Kis ranging between 20 and 298 nM and were extremely potent inhibitors of hCA XII isoenzyme (Kis ranging between 4.3 and 432 nM). Since hCA IX and XII are the cancer-related isoforms recently validated as drug targets, these results represent an important goal in the development of new anticancer candidates. Finally, a computational approach has been performed to better correlate the biological data to the binding mode of these inhibitors.en
dc.identifier10.1080/10520295.2018.1442020
dc.identifier.citationD-ASCENZIO M., GUGLIELMI P., CARRADORI S., SECCI D., FLORIO R., MOLLICA A., CERUSO M., Akdemir A., SOBOLEV A., SUPURAN C., -Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms.-, Journal of enzyme inhibition and medicinal chemistry, cilt.32, ss.51-59, 2017
dc.identifier.doi10.1080/14756366.2016.1235040
dc.identifier.pubmed27784170
dc.identifier.scopus84992390041
dc.identifier.urihttps://hdl.handle.net/20.500.12645/8291
dc.identifier.wosWOS:000392591100044
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.titleOpen saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms.
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameBIOTECHNIC & HISTOCHEMISTRY
local.avesis.idce777b6f-2440-4ac3-9341-4f19cea57dcc
local.avesis.response8167
local.publication.goal03 - Sağlık ve Kaliteli Yaşam
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isGoalOfPublication9c198c48-b603-4e2f-8366-04edcfc1224c
relation.isGoalOfPublication.latestForDiscovery9c198c48-b603-4e2f-8366-04edcfc1224c
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