Synthesis and biological activity of the intercalating agent 3-acetamido-5-[123/125I]iodo-6-aminoacridine.
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.
Kinsey
B M
BM
Department of Radiology (Nuclear Medicine), Harvard Medical School, Boston, MA 02115.
Fayad
F
F
Venkateshan
C N
CN
Adelstein
S J
SJ
Kassis
A I
AI
D000166:Acridines / Q000138:chemical synthesis*; D004247:DNA / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D007457:Iodine Radioisotopes / Q000627:therapeutic use; D007553:Isotope Labeling; D008297:Male; D011370:Proflavine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D011471:Prostatic Neoplasms / Q000378:metabolism / Q000532:radiotherapy
D000166:Acridines; D007364:Intercalating Agents; D007457:Iodine Radioisotopes; C059684:3-acetamido-5-iodoproflavine; D004247:DNA; D011370:Proflavine