title: Design, synthesis and initial characterisation of a radiolabelled [(18)F]pyrimidoindolone probe for detecting activated caspase-3/7.
abstract: 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.
authors: Comprehensive Cancer Imaging Centre, Department of Surgery and Cancer, Imperial College London, Hammersmith Campus, Du Cane Road, London, W12 0NN, UK. e.aboagye@imperial.ac.uk.
authors: A
authors: A
authors: Udemba
authors: G
authors: G
authors: Smith
authors: Q-D
authors: QD
authors: Nguyen
authors: M
authors: M
authors: Kaliszczak
authors: L
authors: L
authors: Carroll
authors: R
authors: R
authors: Fortt
authors: M J
authors: MJ
authors: Fuchter
authors: E O
authors: EO
authors: Aboagye
mesh_terms: D000480:Alkynes / Q000138:chemical synthesis / Q000737:chemistry; D000818:Animals; D018938:Caco-2 Cells; D053148:Caspase 3 / Q000378:metabolism*; D053179:Caspase 7 / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004789:Enzyme Activation; D006801:Humans; D007211:Indoles / Q000097:blood / Q000138:chemical synthesis* / Q000737:chemistry / Q000652:urine; D020128:Inhibitory Concentration 50; D008099:Liver / Q000378:metabolism; D051379:Mice; D008954:Models, Biological; D011743:Pyrimidines / Q000097:blood / Q000138:chemical synthesis* / Q000737:chemistry / Q000652:urine; D014018:Tissue Distribution
chemical_list: C000604634:8'-(2-(((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methoxy)methyl)pyrrolidin-1-ylsulfonyl)-2'H-spiro(cyclopentane-1,3'-pyrimido(1,2-a)indol)-10'(4'H)-one; D000480:Alkynes; D007211:Indoles; D011743:Pyrimidines; D053148:Caspase 3; D053179:Caspase 7