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

Senait Ghirmai, Eskender Mume, Hans Lundqvist, Vladimir Tolmachev, Stefan Sjöberg

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)855-871
Number of pages17
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume48
Issue number12
DOIs
Publication statusPublished - 30 Oct 2005
Externally publishedYes

Keywords

  • 9-aminoacridine derivatives
  • I
  • Chloramine-T
  • Radioiodination

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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