Synthesis and radioiodination of some 9‐aminoacridine derivatives for potential use in radionuclide therapy | Zendy

Ghirmai Senait | Zendy; Mume Eskender | Zendy; Lundqvist Hans | Zendy; Tolmachev Vladimir | Zendy; Sjöberg Stefan | Zendy

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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.

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