Rapid microwave-enhanced synthesis of C5-alkynyl pyranonucleosides as novel cytotoxic antitumor agents

A microwave-assisted, one-pot, coupling reaction for the synthesis of C5-alkynyl-uracil and cytosine glucopyranonucleosides has been developed. Among them, 5-phenylethynyluracil pyranonucleoside derivative 6a, effectively inhibited tumor cell proliferation (IC50 of 5.2-6.2 μM).