Synthesis and radioiodination of some 9-aminoacridine derivatives for potential use in radionuclide therapy

Three derivatives of the DNA intercalating compound 9‐aminoacridine, were prepared and radioiodinated for biological experiments. The compounds are the stannyl derivatives 3‐{4‐[3‐(acridin‐9‐ylamino)‐propoxy]‐3‐trimethylstannyl‐phenyl}‐propionic acid and acridin‐9‐yl‐{3‐[4‐(2‐amino‐ethyl)‐2‐trimethy...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2005-10, Vol.48 (12), p.855-871
Main Authors: Ghirmai, Senait, Mume, Eskender, Lundqvist, Hans, Tolmachev, Vladimir, Sjöberg, Stefan
Format: Article
Language:English
Subjects:
125I
9-aminoacridine derivatives
Biological and medical sciences
Chemistry
chloramine-T
Contrast media. Radiopharmaceuticals
Kemi
Medical sciences
NATURAL SCIENCES
NATURVETENSKAP
Organic chemistry
Organisk kemi
Pharmacology. Drug treatments
radioiodination
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Summary:Three derivatives of the DNA intercalating compound 9‐aminoacridine, were prepared and radioiodinated for biological experiments. The compounds are the stannyl derivatives 3‐{4‐[3‐(acridin‐9‐ylamino)‐propoxy]‐3‐trimethylstannyl‐phenyl}‐propionic acid and acridin‐9‐yl‐{3‐[4‐(2‐amino‐ethyl)‐2‐trimethylstannyl‐phenoxy]‐propyl}‐amine which were synthesized from the corresponding iodo derivatives by palladium catalyzed reactions, and 4‐[2‐(acridin‐9‐ylamino)‐ethyl]‐phenol. The two stannylated compounds and the phenol were used as precursors for radioiodination and were labeled with 125I using chloramine‐T as an oxidant achieving high‐to‐excellent yields. Copyright © 2005 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
1099-1344
DOI:10.1002/jlcr.960