Strategies for the design and synthesis of boronated nucleic acid and protein components as potential delivery agents for neutron capture therapy

Journal Article · Wed Mar 30 00:00:00 EST 1994 · International Journal of Radiation Oncology, Biology and Physics; (United States)

DOI:https://doi.org/10.1016/0360-3016(94)90495-2· OSTI ID:6768213

Wyzlic, I M; Tjarks, W; Soloway, A H; Anisuzzaman, A K.M.; Rong, Feng-Guang; Barth, R F ^[1]

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1. Ohio State Univ., Columbus, OH (United States)

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. 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 [mu]g [sup 10]B/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. 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. Boronated nucleosides, amino acids and peptides can be considered as potential targeting agents for BNCT. 96 refs., 4 figs.

• DOE Contract Number: FG02-90ER60972
• OSTI ID: 6768213
• Journal Information: International Journal of Radiation Oncology, Biology and Physics; (United States), Vol. 28:5; ISSN 0360-3016
• Country of Publication: United States
• Language: English

Related Subjects

37 INORGANIC
ORGANIC
PHYSICAL AND ANALYTICAL CHEMISTRY
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINO ACIDS
DERIVATIZATION
BORON COMPOUNDS
CHEMICAL PREPARATION
NUCLEOSIDES
NUCLEOTIDES
PEPTIDES
CARBOXYLIC ACIDS
CHEMICAL REACTIONS
ORGANIC ACIDS
ORGANIC COMPOUNDS
PROTEINS
RIBOSIDES
SYNTHESIS
400201* - Chemical & Physicochemical Properties
550603 - Medicine- External Radiation in Therapy- (1980-)