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Direct lithiation of 1-(2-tetrahydrofuryl)-5-fluorouracil (Ftorafur) has been investigated. The treatment of ftorafur with lithium diisopropylamide (LDA)at -70 in ether-hexane, followed by the reaction with various electrophiles afforded the corresponding 6-substituted silicon, germanium and tin derivatives of ftorafur. The results of biological investigation indicate the ability of germanium-modified nucleoside analogues to interfere with transcription and replication processes.

metal-based drugs

Synthesis, Structure and Biological Activity of 6-<mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" id="E1"><mml:msub><mml:mtext>R</mml:mtext><mml:mn>3</mml:mn></mml:msub></mml:math>Si(Ge, Sn)-Substituted 5-Fluorouracils

Synthesis, Structure and Biological Activity of 6-R3Si(Ge, Sn)-Substituted 5-Fluorouracils