Synthesis of new carbon-11-labeled 7-aroylaminoindoline-1-sulfonamides as potential PET agents for imaging of tubulin polymerization in cancers

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

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

The tubulin polymerization is an attractive target for anticancer therapy and in the development of cancer imaging agents for use in biomedical imaging technique positron emission tomography (PET). 7-Aroyl-aminoindoline-1 -sulfonamides are a novel class of potent antitublin agents. Carbon-11 -labeled 7-aroyl-aminoindoline-1-sulfonamides have been synthesized as new potential PET agents for imaging of tubulin polymerization in cancers. The target tracers were prepared by O-[11C]methylation of their corresponding precursors using [11C]CH3OTf and isolated by a simplified solid-phase extraction purification procedure in 40-55% radiochemical yields based on [11C]CO2 and decay corrected to the end of bombardment (EOB), 15-20 min overall synthesis time from EOB, >98% radiochemical purity, and 74-111 GBq/μmol specific activity at the end of synthesis.

Original languageEnglish (US)
Pages (from-to)6-11
Number of pages6
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume51
Issue number1
DOIs
StatePublished - Jan 1 2008

Keywords

  • 7-aroyl-aminoindoline-1-sulfonamides
  • Cancer imaging
  • Carbon-11
  • PET
  • Tubulin polymerization

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

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