Strategies for the design and synthesis of boronated nucleic acid and protein components as potential delivery agents for neutron capture therapy.
OBJECTIVE
Strategies for the design and synthesis of boronated nucleosides, amino acids, and peptides as potential delivery agents for boron neutron capture therapy (BNCT) are described.


METHODS
For BNCT to be a useful treatment modality, there is a need to design and synthesize nontoxic boron compounds that selectively target tumor cells, accumulate in sufficient amounts (20-30 micrograms 10B/g of tumor) and persist at therapeutic levels for a sufficient time prior to neutron irradiation. Boronated nucleosides, amino acids and peptides are such promising target compounds. Such structures may be selectively used by proliferating neoplastic cells compared with mitotically less active normal cells and therefore achieve the tissue differentials necessary for BNCT.


RESULTS
The rationale for synthesis of boronated nucleic acid and protein components is discussed. Results of biological and clinical studies of some boronated nucleosides, nucleotides, amino acids and peptides are presented.


CONCLUSIONS
Boronated nucleosides, amino acids and peptides can be considered as potential targeting agents for BNCT.
Wyzlic
I M
IM
College of Pharmacy, Ohio State University, Columbus 43210.
Tjarks
W
W
Soloway
A H
AH
Anisuzzaman
A K
AK
Rong
F G
FG
Barth
R F
RF
D001896:Boron Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016754:Boron Neutron Capture Therapy; D006801:Humans; D009705:Nucleosides / Q000138:chemical synthesis*; D010455:Peptides / Q000138:chemical synthesis; D011506:Proteins / Q000138:chemical synthesis*; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis*
D001896:Boron Compounds; D009705:Nucleosides; D010455:Peptides; D011506:Proteins; D011838:Radiation-Sensitizing Agents