Radioiodination and preliminary biological tests of aniline-mustard and its glucuronide conjugate as a potential anticancer prodrug


UNAK T., Akgun Z. E. , DUMAN Y., YILDIRIM Y. , AVCIBASI U., CETINKAYA B.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, cilt.256, ss.529-534, 2003 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 256 Konu: 3
  • Basım Tarihi: 2003
  • Doi Numarası: 10.1023/a:1024564102831
  • Dergi Adı: JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • Sayfa Sayıları: ss.529-534

Özet

Aniline-mustard and its glucuronide conjugate were radioiodinated with I-131. The preliminary dynamic tests were carried out on rabbits. The scintigrams showed clearly that the glucuronide conjugate of aniline-mustard was very quickly cleared from the metabolism, accumulating in the bladder in about 15 minutes. The clearance time of radioiodinated aniline-mustard-glucuronide was considerably longer (about 45 min.). The results obtained from the biodistributional studies have represented interesting differences between the metabolic details of radioiodinated compounds, and indicated that the glucuronide conjugate of aniline-mustard may be a promising radioiodinated prodrug, if verification of its selective accumulation in some kinds of tumor cells can be obtained.