title: The effect of the [18F]-PEG group on tracer qualification of [4-(phenylamino)-quinazoline-6-YL]-amide moiety--an EGFR putative irreversible inhibitor.
abstract: Previous reports have designated the labeled derivatives of [4-(phenylamino)-quinazoline-6-yl]-amide group as the most promising EGFR-PET imaging agent candidates. To further improve tracer qualifications and increase stability and solubility, additional derivatives of this group substituted at the 7-position with various lengths of fluoro-polyethyleneglycol (F-PEG) chains were synthesized. These novel derivatives inhibited EGFR autophosphorylation with IC(50) values of 5-40 nM. The compounds were successfully labeled with fluorine-18 at the PEG chain via a three-step radiosynthesis route. The labeled final products were obtained with a 13-32% decay corrected radiochemical yield, 99% radiochemical purity, and high specific activity.
authors.affiliation: Department of Medical Biophysics and Nuclear Medicine, Hadassah Hebrew University, Hadassah University Hospital, POB 12000, Jerusalem 91120, Israel.
authors.forename: Samar
authors.initials: S
authors.lastname: Dissoki
authors.forename: Yoel
authors.initials: Y
authors.lastname: Aviv
authors.forename: Desideriu
authors.initials: D
authors.lastname: Laky
authors.forename: Galith
authors.initials: G
authors.lastname: Abourbeh
authors.forename: Alexander
authors.initials: A
authors.lastname: Levitzki
authors.forename: Eyal
authors.initials: E
authors.lastname: Mishani
mesh_terms: D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000737:chemistry*; D005462:Fluorine Radioisotopes; D010766:Phosphorylation; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D005462:Fluorine Radioisotopes; D011799:Quinazolines; D019275:Radiopharmaceuticals; D011092:Polyethylene Glycols; D066246:ErbB Receptors