A series of novel 2,6‐disubstituted purine derivatives were designed and synthesized from 2,6‐dichloropurine. The structures of target compounds were determined by 1H‐NMR, 13C‐NMR, and HRMS. The synthesized compounds were evaluated for their inhibitory activities against lung cancer cell lines of A549 and liver cancer cell lines of Bel‐7402. 2‐(4‐Benzyloxy‐phenylamino)‐6‐(cyclohexylamino)purine(3), 2‐(4‐chloro‐phenylamino)‐6‐(n‐butylamino)purine (5), 2‐(4‐morpholinoamino)‐6‐(4‐hydroxy‐phenylamino)purine (9), and 2‐(4‐O‐galactosyl‐phenylamino)‐6‐(cyclohexylamino)purine (12) exhibited moderate inhibitory activity.
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