Synthesis and in vivo imaging of a 18F-labeled PARP1 inhibitor using a chemically orthogonal scavenger-assisted high-performance method Academic Article uri icon

Overview

MeSH Major

  • Enzyme Inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Radiopharmaceuticals

abstract

  • Pedal to the metal: The catalyst-free Diels-Alder cycloaddition of trans-cyclooctene and tetrazine was used to quickly and selectively generate an 18F-labeled AZD2281 derivative from a tetrazine-linked precursor. The probe was tested in biological assays, and its targeted accumulation was confirmed in vivo. This protocol allows the parallel synthesis of a library of potential PET imaging agents in a short time, thus increasing the efficiency of lead compound development. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

publication date

  • February 18, 2011

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3471140

Digital Object Identifier (DOI)

  • 10.1002/anie.201006579

PubMed ID

  • 21328671

Additional Document Info

start page

  • 1922

end page

  • 5

volume

  • 50

number

  • 8