Synthesis of [11C]Iressa as a new potential PET cancer imaging agent for epidermal growth factor receptor tyrosine kinase

https://doi.org/10.1016/j.bmcl.2006.04.080Get rights and content

Abstract

Iressa (Gefitinib) is an orally active inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TK) involved in cell signal transduction processes critical to proliferation, apoptosis, repair, and angiogenesis of cancer cells. [11C]Iressa was first designed and synthesized as a new potential positron emission tomography (PET) cancer imaging agent for EGFR-TK in 30–40% radiochemical yield with 4.0–6.0 Ci/μmol specific activity at end of bombardment (EOB).

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Acknowledgments

This work was partially supported by the Susan G. Komen Breast Cancer Foundation, Breast Cancer Research Foundation and Indiana Genomics Initiative (INGEN) of Indiana University, which is supported in part by Lilly Endowment Inc. The authors thank Dr. Bruce H. Mock, Barbara E. Glick-Wilson, and Michael L. Sullivan for their assistance in production of 11CH3OTf. The referees’ criticisms and editor’s comments for the revision of the manuscript are greatly appreciated.

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