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8-Azaxanthine (1), 3-β-D-ribofuranosyl-8-azaxanthine (2), 3-β-D-ribofuranosyl-8-azaxanthine-5’-monophosphate (3), and 3-β-D-ribofiranosyl-8-azaxanthine-5’-(3-pyridinylcarbonyl)monophosphate (4) were synthesized. The in vitro antitumor activities of the synthesized compounds against P388 mouse leukemia, FM3A mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. 2 with unnatural N-3 and C-1’ glycoside bond had activity against three tumor cell lines and IC50 s of these compounds were 0.05, 0.06, and 0.06 μmol/mL against three tumor cell lines, respectively. But these compounds had no antibacterial activity. IC50 s against U937 human histiocytic lymphoma cells were verified with the structural modification: IC50s of 1, 2, 3, and 4 were 0.33, 0.06, 0.25, and 0.33μmol/mL, respectively.
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