A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis

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dc.contributor.authorKrause-Heuer, AMen_AU
dc.contributor.authorHowell, NRen_AU
dc.contributor.authorMatesic, Len_AU
dc.contributor.authorDhand, Gen_AU
dc.contributor.authorYoung, ELen_AU
dc.contributor.authorBurgess, Len_AU
dc.contributor.authorJiang, CDen_AU
dc.contributor.authorLengkeek, NAen_AU
dc.contributor.authorFookes, CJRen_AU
dc.contributor.authorPham, TQen_AU
dc.contributor.authorSobrio, Fen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorFraser, BHen_AU
dc.date.accessioned2018-09-19T22:51:46Zen_AU
dc.date.available2018-09-19T22:51:46Zen_AU
dc.date.issued2012-11-12en_AU
dc.date.statistics2018-09-18en_AU
dc.description.abstractThirteen compounds in a new class of fluorinated 5-pyrrolidinylsulfonyl isatin derivatives were synthesised that have potent and selective inhibitory activity against effector caspases-3 and -7. With in vivo animal PET imaging studies of cerebral ischemia being planned, N-benzylation with selected para-substituted benzylic halides allowed systematic variation of lipophilicity (logP 1.94–3.31) without decreasing inhibition potency (IC50). From this series the p-methoxybenzyl analogue was selected for initial ‘proof-of-concept’ [18F]-fluoride radiolabelling which proceeded in good yield and purity with no need for a protection/deprotection strategy. © 2013 Royal Society of Chemistryen_AU
dc.identifier.citationKrause-Heuer, A. M., Howell, N. R., Matesic, L., Dhand, G., Young, E. L., Burgess, L. Jiang, C. D., Lengkeek, N. A., Fookes, C. J. R., Pham, T. Q., Sobrio, F., Greguric, I & Fraser, B. H. (2013). A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis. MedChemComm, 4(2), 347-352. doi:10.1039/C2MD20249Ben_AU
dc.identifier.govdoc8780en_AU
dc.identifier.issn2040-2503en_AU
dc.identifier.issue2en_AU
dc.identifier.journaltitleMedChemCommen_AU
dc.identifier.pagination347-352en_AU
dc.identifier.urihttps://doi.org/10.1039/C2MD20249Ben_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9027en_AU
dc.identifier.volume4en_AU
dc.language.isoenen_AU
dc.publisherRoyal Society of Chemistryen_AU
dc.subjectIndolesen_AU
dc.subjectEnzyme inhibitorsen_AU
dc.subjectApoptosisen_AU
dc.subjectCell killingen_AU
dc.subjectIndolesen_AU
dc.subjectIn vivoen_AU
dc.subjectFluorine 18en_AU
dc.subjectPositron computed tomographyen_AU
dc.titleA new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosisen_AU
dc.typeJournal Articleen_AU
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