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

Min Wang, Mingzhang Gao, Kathy Miller, George W. Sledge, Gary Hutchins, Qi-Huang Zheng

Research output: Contribution to journalArticle

10 Citations (Scopus)

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. [11C]MKC-1 ([11C]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 [11C]CO2. The specific activity was 222-296 GBq/μmol at EOB and 111-148 GBq/μmol at the end of synthesis, respectively.

Original languageEnglish
Pages (from-to)763-775
Number of pages13
JournalNuclear Medicine and Biology
Volume37
Issue number7
DOIs
StatePublished - Oct 2010

Fingerprint

Carbon
Maleic Anhydrides
Neoplasms
Positron-Emission Tomography
Cell Cycle
3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
indoleacetamide
indole
maleimide
bisindolylmaleimide

Keywords

  • [C]MKC-1 ([C]Ro 31-7453)
  • Cancer imaging
  • Positron emission tomography
  • Radiosynthesis

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

Cite this

The first design and synthesis of [11C]MKC-1 ([11C]Ro 31-7453), a new potential PET cancer imaging agent. / Wang, Min; Gao, Mingzhang; Miller, Kathy; Sledge, George W.; Hutchins, Gary; Zheng, Qi-Huang.

In: Nuclear Medicine and Biology, Vol. 37, No. 7, 10.2010, p. 763-775.

Research output: Contribution to journalArticle

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