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Please use this identifier to cite or link to this item: http://apo.ansto.gov.au/dspace/handle/10238/9027

Title: A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis
Authors: Krause-Heuera, AM
Howell, NR
Matesic, L
Dhand, G
Young, EL
Burgess, L
Jiang, CD
Lengkeek, NA
Fooke, CJR
Pham, TQ
Sobrio, F
Greguric, I
Fraser, BH
Keywords: Indole
Enzyme inhibitors
Apoptosis
Cell killing
Indoles
In vivo
Fluorine 18
Positron computed tomography
Issue Date: 12-Nov-2012
Publisher: Royal Society of Chemistry
Citation: Krause-Heuer, A. M., Howell, N. R., Matesic, L., Dhand, G., Young, E. L., Burgess, L. Jiang,C. D., Lengkeek, N. A., Fooke, 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: https://doi.org/10.1039/C2MD20249B
Abstract: Thirteen 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 Chemistry
URI: https://doi.org/10.1039/C2MD20249B
http://apo.ansto.gov.au/dspace/handle/10238/9027
ISSN: 2040-2503
Appears in Collections:Journal Articles

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