Synthesis and antitumor activity of ent-kaurene diterpenoids / 中国药科大学学报

Aim: To synthesize the ent-kaurene diterpenoid and its derivatives from natural available stevioside.Methods: The crucial pharmacophore of exo-methylene ketone was designed and the carboxyl group at C-4 was modified.The cytotoxic inhibition activities in vitro of target compounds were evaluated against human cancer cells BEL-7402,HO-8910,MCF-7 and HL-60 by a MTT method.Results and Conclusion: The struc-tures of new target compounds were identified by ~1H NMR,FT-IR and EI-MS.The preliminary experimental re-sults showed that some derivatives of ent-kaurene diterpenoid possessed fair inhibitory activity against tumor cell lines compared with that of their parent steviol.