Abstract：The intermediate, {(3R,4R,6R,6R)-2,2-dimethyl-6-［6-(piperazin-1-yl)-9H-purin-9-yl］ tetrahydrofuro［3,4-d］［1,3］dioxol-4-yl}methanol(4), was synthesized by three steps including adjacent hydroxyl protection, chlorination and introduction of piperazine at N6- position, using adenosine as starting material. Eight novel N6-piperazine substituted adenosine analogues(8a~8h) were synthesized by coupling reaction of 4 with 6a~6h, then deprotection of hydroxyl. The structures were characterized by 1H NMR， 13C NMR and HR-ESI-MS. Biological evaluation showed that 8a~8h exhibited antitumor activities on Hela cells, especially, 2-｛4-［9-(3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-9H-purin-6-yl］-piperazin-1-yl｝-N-(3-fluoro-phenyl)-acetamide(8e) exhibited the strongest inhibitory activity with IC50 of 21.74 μmol·L-1.
2016, Vol. 24 
