Synthesis of carbon-11-labeled tariquidar derivatives as new PET agents for imaging of breast cancer resistance protein (ABCG2).

Abstract

Carbon-11-labeled tariquidar derivatives were first designed and synthesized as new PET agents for imaging of breast cancer resistance protein. The target tracers were prepared by O-[(11)C]methylation of their corresponding acid precursors using [(11)C]CH3OTf under basic conditions and isolated by a simplified solid-phase extraction (SPE) method in 50-60% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15-20 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 111-185 GBq/micromol.

• Authors: Min Wang, David X Zheng, Michael B Luo, Mingzhang Gao, Kathy D Miller, Gary D Hutchins, Qi-Huang Zheng
• Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 68 Issue 6 Pg. 1098-103 (Jun 2010) ISSN: 1872-9800 [Electronic] England
• PMID: 20181488 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)
• Copyright: Copyright 2010 Elsevier Ltd. All rights reserved.

Chemical References

• ABCG2 protein, human
• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters
• Carbon Radioisotopes
• Neoplasm Proteins
• Quinolines
• tariquidar

Topics

• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters (analysis)
• Breast Neoplasms (diagnostic imaging)
• Carbon Radioisotopes
• Female
• Humans
• Isotope Labeling (methods)
• Neoplasm Proteins (analysis)
• Positron-Emission Tomography (methods)
• Quinolines (chemical synthesis)