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|Title: ||A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis|
|Authors: ||Krause-Heuera, AM|
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|
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