Synthesis and anticancer activity of novel C6-piperazine substituted purine steroid–nucleosides analogues

• A novel class of C6-piperazine substituted purine nucleoside analogues was synthesized.
• These compounds contain the modified pyranose-like D ring of the 4-azasteroid moiety.
• Compounds 8b and 9b exhibited significant cytotoxicity on PC-3 cell lines.

Novel C6-piperazine substituted purine nucleoside analogues (2–9) bearing a modified pyranose-like D ring of the 4-azasteroid moiety were efficiently synthesized through nucleophilic substitution at C6 position of the steroid–nucleoside precursors (1) with versatile piperazines. All newly-synthesized compounds were evaluated for their anticancer activity in vitro against Hela, PC-3 and MCF-7 cell lines. Among them, compounds 8b and 9b exhibited significant cytotoxicity on PC-3 cell lines.

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