Synthesis and Biochemical Activity of 5-Tethered Carborane-Containing Pyrimidine Nucleosides as Potential Agents for DNA Incorporation

Abstract

Synthesis and biochemical evaluation of a series of 5-tethered carborane-containing pyrimidine nucleosides have been undertaken. The biochemical studies with human TK demonstrated that these compounds can be phosphorylated to the corresponding 5′-monophosphate and that the most significant conversion occurred when seven atoms were inserted between the carborane cage and the pyrimidine base, and of these the best was the one with saturated ester.