High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging …

…, RB Daniel, Y Rozen, M Shaul, A Levitzki

Index: Mishani, Eyal; Abourbeh, Galith; Jacobson, Orit; Dissoki, Samar; Ben Daniel, Revital; Rozen, Yulia; Shaul, Mazal; Levitzki, Alexander Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5337 - 5348

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Citation Number: 83

Abstract

Previous studies with the anilinoquinazoline epidermal growth factor receptor (EGFR) irreversible inhibitor [11C]-ML03 demonstrated a rapid metabolism of the tracer, which led to its low in vivo accumulation in EGFR overexpressing tumors. To enhance tumor uptake, the chemical structure of the compound was modified, and four new groups of EGFR inhibitors with a wide range of chemical reactivities were synthesized. Chemical reactivity assay of ...