Radiosynthesis and in vivo tumor uptake of 2-deoxy-2-[(18)F]fluoro-myo-inositol.

Abstract:

:Inositols play an important role in membrane lipid metabolism and mitogenic signaling of most cancer cells. There is paucity of data on the distribution of radiolabelled inositols. Based on work previously carried out on 1-deoxy-1-[(18)F]fluoro-scyllo-inositol ([(18)F]2), we began a program of work to label myo-inositol (2-deoxy-2-[(18)F]fluoro-myo-inositol, [(18)F]1), the most abundant inositol in cells. Fluorination of a triflate precursor 4 afforded the desired [(18)F]1 following deprotection with a radiochemical yield of 8% n.d.c. [(18)F]1 showed higher uptake in vivo in a human breast cancer xenograft model, MDA-MB-231, compared to [(18)F]2. Thus, we have developed a new inositol radiotracer that could have utility for studying inositol uptake in tumors.

journal_name

Bioorg Med Chem Lett

authors

Carroll L,Perumal M,Vasdev N,Robins E,Aboagye EO

doi

10.1016/j.bmcl.2012.08.022

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

6148-50

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01011-6

journal_volume

22

pub_type

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