Design, synthesis and initial characterisation of a radiolabelled [(18)F]pyrimidoindolone probe for detecting activated caspase-3/7

Evasion of apoptosis is one of the six initially proposed hallmarks of cancer, and as such, a method to detect apoptosis in a tumour would be of considerable interest in both clinical trials of new cancer therapeutics, as well as for routine patient management. Activation of caspase-3/7 is a key bio...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2015-05, Vol.13 (19), p.5418-5423
Main Authors: Udemba, A, Smith, G, Nguyen, Q-D, Kaliszczak, M, Carroll, L, Fortt, R, Fuchter, M J, Aboagye, E O
Format: Article
Language:English
Subjects:
Alkynes - chemical synthesis
Alkynes - chemistry
Animals
Caco-2 Cells
Caspase 3 - metabolism
Caspase 7 - metabolism
Chromatography, High Pressure Liquid
Enzyme Activation
Humans
Indoles - blood
Indoles - chemical synthesis
Indoles - chemistry
Indoles - urine
Inhibitory Concentration 50
Liver - metabolism
Mice
Models, Biological
Pyrimidines - blood
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - urine
Tissue Distribution
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Summary:Evasion of apoptosis is one of the six initially proposed hallmarks of cancer, and as such, a method to detect apoptosis in a tumour would be of considerable interest in both clinical trials of new cancer therapeutics, as well as for routine patient management. Activation of caspase-3/7 is a key biomarker of cellular apoptosis. Herein we describe the design, synthesis and initial characterisation of the first pyrimidoindolone compound for detection of caspase-3/7 activation using positron emission tomography.
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob00058k