Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp

Marialessandra Contino; Laura Zinzi; Maria Grazia Perrone; Marcello Leopoldo; Francesco Berardi; Roberto Perrone; Nicola Antonio Colabufo

doi:10.1016/j.bmcl.2012.12.084

Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1370-4. doi: 10.1016/j.bmcl.2012.12.084. Epub 2013 Jan 5.

Authors

Marialessandra Contino¹, Laura Zinzi, Maria Grazia Perrone, Marcello Leopoldo, Francesco Berardi, Roberto Perrone, Nicola Antonio Colabufo

Affiliation

¹ Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari 'A. Moro', via Orabona, 4, 70125 Bari, Italy.

PMID: 23374872
DOI: 10.1016/j.bmcl.2012.12.084

Abstract

Compounds 8a-d have been designed as bioisosters of tariquidar for imaging P-gp expression and density by PET. The results displayed that compounds 8b and 8d could be considered potential P-gp/BCRP ligands suitable as (11)C and (18)F radiotracers, respectively.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / analysis*
Carbon Radioisotopes / chemistry
Fluorine Radioisotopes / chemistry
Humans
Positron-Emission Tomography / methods*
Quinolines / chemical synthesis
Quinolines / chemistry*
Radiopharmaceuticals / chemical synthesis
Radiopharmaceuticals / chemistry*
Thiazoles / chemical synthesis
Thiazoles / chemistry

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Carbon Radioisotopes
Fluorine Radioisotopes
Quinolines
Radiopharmaceuticals
Thiazoles
tariquidar