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Synthesis and radioiodination of some 9‐aminoacridine derivatives for potential use in radionuclide therapy
Author(s) -
Ghirmai Senait,
Mume Eskender,
Lundqvist Hans,
Tolmachev Vladimir,
Sjöberg Stefan
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.960
Subject(s) - chemistry , phenol , amine gas treating , chloramine t , radionuclide therapy , medicinal chemistry , organic chemistry , combinatorial chemistry , medicine , nuclear medicine
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 125 I using chloramine‐T as an oxidant achieving high‐to‐excellent yields. Copyright © 2005 John Wiley & Sons, Ltd.