The use of boron clusters in the rational design of boronated nucleosides for neutron capture therapy of cancer

Boron neutron capture therapy (BNCT) is a chemoradio-therapeutic method for the treatment of cancer. It depends on the selective targeting of tumor ce lls by boron-containing compounds. One category of BNCT agents that has rec eived extensive attention during recent years is boronated nucleosides. Suc h structures may be converted to the corresponding 5'-monophosphates by pho sphorylating enzymes and thereby entrapped in tumor cells by the virtue of the acquired negative charge. This review analyzes previous design strategi es applied in the synthesis of boron cluster-containing nucleosides and dis cusses possible future developments in this field based on existing knowled ge of enzyme tissue expressions, enzyme substrate specificities, and contem porary trends in rational drug design. (C) 2000 Elsevier Science B.V. All r ights reserved.