Article

The first design and synthesis of [11C]MKC-1 ([11C]Ro 31-7453), a new potential PET cancer imaging agent.

Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Nuclear Medicine and Biology (impact factor: 3.02). 10/2010; 37(7):763-75. DOI:10.1016/j.nucmedbio.2010.04.186 pp.763-75
Source: PubMed

ABSTRACT Bisindolylmaleimide MKC-1 (formerly known as Ro 31-7453) is a novel, orally active, small-molecule, cell cycle inhibitor with broad-spectrum antitumor effects. [(11)C]MKC-1 ([(11)C]Ro 31-7453) was first designed and synthesized as a new potential positron emission tomography cancer imaging agent through two different strategies. The first strategy was to prepare a carbon-11-labeled bisindolyl maleic anhydride intermediate followed by the conversion to maleimide. The second strategy involved the condensation of either carbon-11-labeled indole-3-acetamides with indole-3-glyoxalates, or indole-3-acetamides with carbon-11-labeled indole-3-glyoxalates. The radiochemical yields were 15-30%, decay corrected to end of bombardment (EOB), based on [(11)C]CO(2). The specific activity was 222-296 GBq/μmol at EOB and 111-148 GBq/μmol at the end of synthesis, respectively.

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Data provided are for informational purposes only. Although carefully collected, accuracy cannot be guaranteed. The impact factor represents a rough estimation of the journal's impact factor and does not reflect the actual current impact factor. Publisher conditions are provided by RoMEO. Differing provisions from the publisher's actual policy or licence agreement may be applicable.

Keywords

Bisindolylmaleimide MKC-1
 
broad-spectrum antitumor effects
 
carbon-11-labeled bisindolyl maleic anhydride intermediate
 
cell cycle inhibitor
 
condensation
 
maleimide
 
new potential positron emission tomography cancer imaging agent
 
orally active
 
radiochemical yields
 
specific activity
 
synthesized