Evaluation of EGFR-TK Expression with a ^99mTc-Labeled Complex Bearing Quinazoline Pharmacophore

Abstract

Objectives: The epidermal growth factor receptor (EGFR) signaling pathway is widely recognized to play an important role in development and progression of many malignant tumors, including lung cancer. The aim of this study was to produce a useful technetium-99m (99m Tc) complex for early detection and staging of EGFRpositive tumors. Methods: The authors labeled quinazoline derivative (3-iodinephenyl) quinazoline-4, 6-diamine with 99m Tc using S-acetylmercaptoacetyltriglyglycinate (MAG 3) conjugated to quinazoline derivative through 4-[(2aminoethyl)amino]-4-oxobut-2-enoic acid because it is a bifunctional chelator with an average yield of 93.9%-2.5% and radiochemical purity of >98%. Results: In vitro studies indicate that the [ 99m Tc]-complex 13 has high stability in physiological conditions and binds the HCC 827 cells and shows HCC 827 internalization. The biodistribution of the [ 99m Tc]-complex 13 in healthy Institute of Cancer Research mice indicates the rather fast blood clearance through the hepatobiliary system. Conclusion: These preliminary results pave the road for estimating the status of EGFR and monitoring the response to EGFR tyrosine kinase inhibitors as a personalized cancer therapy regimen.

Synthesis and Biological Evaluation of 99mTc-Labeled Phenylpiperazine Derivatives as Selective Serotonin-7 Receptor Ligands for Brain Tumor Imaging

“…It can be due to the high affinity and rapid clearance from blood and nontarget tissues of 99m Tc-MPHH, which increases the contrast images by reducing the background (Table , Figure ). − …”

Evaluation of Rhenium and Technetium-99m Complexes Bearing Quinazoline Derivatives as Potential EGFR Agents

“…In the majority of the reported 99m Tc-labeled quinazoline derivatives [ 10 , 11 , 12 , 13 ], the 4-anilinoquinazoline pharmacophore was coupled to tailor-made chelators suitable for the stabilization of either the M III (M = Re and 99m Tc) core with a ‘‘4+1′’ mixed-ligand system or the tricarbonyl fac -[M I (CO) 3 ] + core. It was shown that the presence of the organometallic core does not deteriorate the pharmacological properties of the 4-anilinoquinazoline pharmacophore.…”