Evaluation of 18F-labeled icotinib derivatives as potential PET agents for tumor imaging
In this study, three 18F-labeled crown ether fused anilinoquinazoline derivatives ([18F]11a–c) were synthesized and evaluated as potential tumor imaging probes. The biodistribution results of [18F]11b were good. Compared with [18F]-fludeoxyglucose and l-[18F]-fluoroethyltyrosine in the same animal model, [18F]11b had better tumor/brain, tumor/muscle, and tumor/blood uptake ratios. Overall, these results suggest that [18F]11b is promising as a tumor imaging agent for positron emission tomography.
KeywordsQuinazoline derivatives Biodistribution 18F PET
We conducted this work with financial support from The National Natural Science Foundation of China (No. 21071022) and the Fundamental Research Funds for the Central Universities. In addition, we would like to thank the cyclotron operator team of the PET center of Xuanwu Hospital for providing the fluoride-18 nuclide.
- 3.Block MH (1992) The aminoquinazoline group as a replacement for the salicylamide group: the design and synthesis of a novel highly selective beta 1 adrenoceptor partial agonist. Drug Des Discov 9:167–176Google Scholar
- 4.Ciardiello F (2000) Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin Cancer Res 6:2053–2063Google Scholar
- 7.Ren X (2005) Research progresses of epidermal growth factor receptor tyrosine kinase inhibitors. Chin J New Drugs 14:821–826Google Scholar
- 11.Mei DAI (2009) EGFR-targeted agents in cancer therapy. Chin Bull Life Sci 21:412–417Google Scholar
- 14.Minkovsky N (2008) BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors. Curr Opin Investig Drugs 9:1336–1346Google Scholar
- 24.Yang Y (2012) Application status and prospect of domestic drug: icotinib. J Pract Med 28(23):4016–4018Google Scholar
- 26.Wang, YX (2011) Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof. US20110182882[P]Google Scholar