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

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4102-6. doi: 10.1016/j.bmcl.2006.04.080. Epub 2006 May 11.

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/micromol specific activity at end of bombardment (EOB).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • ErbB Receptors / antagonists & inhibitors*
  • Gefitinib
  • Humans
  • Neoplasms / diagnosis*
  • Neoplasms / enzymology
  • Positron-Emission Tomography*
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology

Substances

  • Antineoplastic Agents
  • Quinazolines
  • ErbB Receptors
  • Gefitinib