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.
Marialessandra Contino  1 ,  Laura Zinzi ,  Maria Grazia Perrone ,  Marcello Leopoldo ,  Francesco Berardi ,  Roberto Perrone ,  Nicola Antonio Colabufo
Affiliations
  • 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.