Synthesis of carbon-11-labeled tariquidar derivatives as new PET agents for imaging of breast cancer resistance protein (ABCG2).
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.
Wang
Min
M
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202, USA.
Zheng
David X
DX
Luo
Michael B
MB
Gao
Mingzhang
M
Miller
Kathy D
KD
Hutchins
Gary D
GD
Zheng
Qi-Huang
QH
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000032:analysis*; D001943:Breast Neoplasms / Q000000981:diagnostic imaging*; D002250:Carbon Radioisotopes; D005260:Female; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D009363:Neoplasm Proteins / Q000032:analysis*; D049268:Positron-Emission Tomography / Q000379:methods; D011804:Quinolines / Q000138:chemical synthesis*
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D002250:Carbon Radioisotopes; D009363:Neoplasm Proteins; D011804:Quinolines; C402343:tariquidar