SYNTHESIS AND BIOCHEMICAL-ACTIVITY OF 5-TETHERED CARBORANE-CONTAININGPYRIMIDINE NUCLEOSIDES AS POTENTIAL AGENTS FOR DNA INCORPORATION

Synthesis and biochemical evaluation of a series of 5-tethered carbora ne-containing pyrimidine nucleosides have been undertaken. The biochem ical studies with human TK demonstrated that these compounds can be ph osphorylated to the corresponding 5'-monophosphate and that the most s ignificant 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.