Radiolabelling of the potential anti‐cancer agent, 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) with fluorine‐18

doi:10.1002/JLCR.25804401132

Paper

Radiolabelling of the potential anti‐cancer agent, 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) with fluorine‐18

Published May 1, 2001 · G. Brown, H. Wilson, A. Westwell

Journal of Labelled Compounds and Radiopharmaceuticals

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Abstract

The novel potential antitumour agent 5-fluoro-2-(4-amino-3-methylphenyl)benzothiazole (5F203) has been radiolabelled with fluorine-18 by reaction of an amino protected trimethyltin precursor with molecular fluorine (18F-F) followed by alkaline deprotection of the amino group. [18F]5F203 was obtained in ca 10% radiochemical yield in ca. 60 mins from end of bombardment.

Study Snapshot

The radiolabelling of 5-fluoro-2-(4-amino-3-methylphenyl)benzothiazole (5F203) with fluorine-18 provides a potential anti-cancer agent with a radiochemical yield of ca 10% within 60 minutes.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Radiolabelling of the potential anti‐cancer agent, 5‐fluoro‐2‐(4‐amino‐3‐methylphenyl)benzothiazole (5F203) with fluorine‐18

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References

The regiospecific synthesis of 5- and 7-monosubstituted and 5,6-disubstituted 2-arylbenzothiazoles†

This study presents a regiospecific synthesis method for antitumor 2-arylbenzothiazoles, using bromine as a guide for cyclization, producing a mixture of regioisomers.

Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.

The novel antitumor agent 2-(4-aminophenyl)benzothiazole (1a) selectively inhibits growth of sensitive breast cancer cell lines MCF-7 and T-47D, with its mechanism of action likely dependent on differential metabolism and intracellular protein binding.

2-(4-Aminophenyl)benzothiazoles: novel agents with selective profiles of in vitro anti-tumour activity.

2-(4-aminophenyl)benzothiazoles show unique growth inhibition profiles in vitro, targeting various cancer cell lines with unique modes of action.

Citations

Antitumour properties of fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones ('quinols').

Fluorinated benzothiazole-substituted hydroxycyclohexa-2,5-dienones show comparable antitumor activity to non-fluorinated precursor PMX 464, with potential for future cancer treatments.