Synthesis and preliminary biological evaluation of MMP inhibitor radiotracers [11C]methyl-halo-CGS 27023A analogs, new potential PET breast cancer imaging agents

Qi Huang Zheng, Xiangshu Fei, Xuan Liu, Ji Quan Wang, Hui Bin Sun, Bruce H. Mock, K. Lee Stone, Tanya D. Martinez, Kathy D. Miller, George W. Sledge, Gary D. Hutchins

Research output: Contribution to journalArticle

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A series of [11C]methyl-halo-CGS 27023A analogs (2-F, 1a; 4-F, 1b; 2-Cl, 1c; 3-Cl, 1d; 4-Cl, 1e; 2-Br, 1f; 3-Br, 1g; 4-Br, 1h; 4-I, 1i), novel radiolabeled matrix metalloproteinase (MMP) inhibitors, have been synthesized for evaluation as new potential positron emission tomography (PET) breast cancer imaging agents. The precursors halo-CGS 27023A analogs (2-F, 6a; 4-F, 6b; 2-Cl, 6c; 3-Cl, 6d; 4-Cl, 6e; 2-Br, 6f; 3-Br, 6g; 4-Br, 6h; 4-I, 6i) for radiolabeling were obtained in four steps from starting material amino acid D-valine with moderate to excellent chemical yields. Precursors were labeled by [11C]methyl triflate through 11C-O-methylation method at the aminohydroxyl position under basic conditions and isolated by solid-phase extraction (SPE) purification to produce pure target compounds in 40-60% radiochemical yields (decay corrected to end of bombardment), in 20-25 min synthesis time.

Original languageEnglish (US)
Pages (from-to)761-770
Number of pages10
JournalNuclear Medicine and Biology
Issue number7
StatePublished - Oct 1 2002



  • [C]Methyl-halo-CGS 27023A analogs
  • Breast cancer
  • Carbon-11
  • Matrix metalloproteinase inhibitor
  • Positron emission tomography
  • Radiotracer

ASJC Scopus subject areas

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

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