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

…, MG Perrone, M Leopoldo, F Berardi, R Perrone…

Index: Contino, Marialessandra; Zinzi, Laura; Perrone, Maria Grazia; Leopoldo, Marcello; Berardi, Francesco; Perrone, Roberto; Colabufo, Nicola Antonio Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1370 - 1374

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Citation Number: 4

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. ... In our laboratory, MC18 and MC113 have been designed as P-gp ligands and their biological evaluation classified them as potent and selective P-gp inhibitors; 8 and 9 thus, these ligands have been [ 11 ...