Synthesis and biological activity of a boron-containing pyrimidine nucleoside

The potential of purine and pyrimidine nucleoside analogs for the chemotherapy of viruses and cancers has been well recognized. These compounds behave as substitutes of natural components of nucleic acids and co-enzymes, and they have been extensively reviewed. Various boron heterocycles which resemble the bases of DNA have been tested for anticancer activity, but most of these have been found to be either hydrolytically and biologically unstable or too toxic. The authors approach was to synthesize a boron-containing nucleoside which closely resembles one of the naturally occurring pyrimidine nucleosides. This compound could be taken up selectively by tumors and be preferentially trapped in the cell. In addition, neutron irridiation of the cells containing this boron nucleoside could result in cell destruction