Study on fluorine-and/or boron-containing amino acids and their related compounds as tools for diagnosis and treatment of cancer

摘要

According to a preliminary elucidation,dipeptides containing 3-(4-fluorophenyl)-alanine [Phe(F)] seem to be transferred into some kinds of tumor cells through the oligopeptide transporter.This fact suggests that the magnetic resonance imaging(MRI)based on ~(19)F NMR measurement of the Phe(F)-containing peptides internalized into the tumor cells may be accessible as a promising means for diagnosis of cancer.From the standpoint of a treatment of brain cancer or melanoma,the boron neutron capture therapy(BNCT)based on the interaction of ~(10)B isotope and neutron has been highly noted in recent years.In order to develop practical tools for MRI and BNCT,we designed and synthesized a series of dipeptides or dipeptidomimetics composed of fluorine-or boron-containing compounds as well as the novel compounds containing both fluorine and boron atoms in a single molecule.