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

✍ Scribed by Senait Ghirmai; Eskender Mume; Hans Lundqvist; Vladimir Tolmachev; Stefan Sjöberg

• Publisher: John Wiley and Sons
• Year: 2005
• Tongue: French
• Weight: 175 KB
• Volume: 48
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.960

✦ Synopsis

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-toexcellent yields.