STRATEGIES FOR THE DESIGN AND SYNTHESIS OF BORONATED NUCLEIC-ACID ANDPROTEIN-COMPONENTS AS POTENTIAL DELIVERY AGENTS FOR NEUTRON-CAPTURE THERAPY

Purpose: Strategies for the design and synthesis of boronated nucleosi des, amino acids, and peptides as potential delivery agents for boron neutron capture therapy (BNCT) are described. Methods and Materials: F or BNCT to be a useful treatment modality, there is a need to design a nd synthesize nontoxic boron compounds that selectively target tumor c ells, accumulate in sufficient amounts (20-39 mu g B-10/g of tumor) an d 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 b y 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 a cid and protein components is discussed. Results of biological and cli nical studies of some boronated nucleosides, nucleotides, amino acids and peptides are presented. Conclusion: Boronated nucleosides, amino a cids and peptides can be considered as potential targeting agents for BNCT.