Identification, development, synthesis and evaluation of boron-containing nucleosides for neutron capture therapy

The development of boron compounds with the capacity for selectively target ing tumor cells would offer the potential for specifically destroying such cells using the capture reaction of the nonradioactive B-10 nuclide and the rmal neutrons. The key problem is the development of compounds with the abi lity to discriminate between tumor cells and contiguous normal cells and to concentrate in the former at suitable concentration levels. One category o f agents that has been explored is boron-containing nucleosides. Such recen t structures have been biochemically converted in vitro to their correspond ing nucleotides by the action of human thymidine kinase. These studies have attempted to correlate a compound's physiochemical properties with its bio chemical attributes. Since only a fraction of cells are undergoing replicat ion at any one time, requiring the need for nucleic acid precursors, such b oron compounds must be only one component of a cocktail of agents that are targeting malignant cells. This presentation is selective, focusing on thos e boron-containing nucleosides that have been designed for studies with kin ases. (C) 1999 Elsevier Science S.A. All rights reserved.