Synthesis and biological evaluation of an 18fluorine-labeled COX inhibitor - [18F]fluorooctyl fenbufen amide - For imaging of brain tumors

4Citations
Citations of this article
11Readers
Mendeley users who have this article in their library.

Abstract

Molecular imaging of brain tumors remains a great challenge, despite the advances made in imaging technology. An anti-inflammatory compound may be a useful tool for this purpose because there is evidence of inflammatory processes in brain tumor micro-environments. Fluorooctylfenbufen amide (FOFA) was prepared from 8-chlorooctanol via treatment with potassium phthalimide, tosylation with Ts2O, fluorination with KF under phase transfer catalyzed conditions, deprotection using aqueous hydrazine, and coupling with fenbufen. The corresponding radiofluoro product [18F]FOFA, had a final radiochemical yield of 2.81 mCi and was prepared from activated [18F]F- (212 mCi) via HPLC purification and concentration. The radiochemical purity was determined to be 99%, and the specific activity was shown to exceed 22 GBq/μmol (EOS) based on decay-corrected calculations. Ex-vivo analysis of [18F]FOFA in plasma using HPLC showed that the agent had a half-life of 15 min. PET scanning showed significant accumulation of [18F]FOFA over tumor loci with reasonable contrast in C6-glioma bearing rats. These results suggest that this molecule is a promising agent for the visualization of brain tumors. Further investigations should focus on tumor micro-environments.

Cite

CITATION STYLE

APA

Huang, Y. C., Chang, Y. C., Yeh, C. N., & Yu, C. S. (2016). Synthesis and biological evaluation of an 18fluorine-labeled COX inhibitor - [18F]fluorooctyl fenbufen amide - For imaging of brain tumors. Molecules, 21(3). https://doi.org/10.3390/molecules21030387

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free