Synthesis and biological activity of the intercalating agent 3-acetamido-5-[123/125I]iodo-6-aminoacridine

Int J Rad Appl Instrum B. 1990;17(3):341-6. doi: 10.1016/0883-2897(90)90062-6.

Abstract

3-Acetamido-5-iodo-6-aminoacridine (3), a derivative of the known intercalating agent proflavine (3,6-diaminoacridine) (1) was synthesized, and no-carrier-added 123I and 125I labeled compounds prepared. Compound 3 was taken up by live cells and localized in the nucleus. The intracellular concentration of [125I]3 was 7-fold greater in human prostate carcinoma (PC-3) cells than in normal Chinese hamster lung fibroblast (V-79) cells.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acridines / chemical synthesis*
  • DNA / metabolism
  • Humans
  • In Vitro Techniques
  • Intercalating Agents / chemical synthesis*
  • Intercalating Agents / metabolism
  • Intercalating Agents / pharmacokinetics
  • Iodine Radioisotopes / therapeutic use
  • Isotope Labeling
  • Male
  • Proflavine / analogs & derivatives
  • Proflavine / chemical synthesis*
  • Proflavine / metabolism
  • Proflavine / pharmacokinetics
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / radiotherapy

Substances

  • Acridines
  • Intercalating Agents
  • Iodine Radioisotopes
  • 3-acetamido-5-iodoproflavine
  • DNA
  • Proflavine