Objective To synthesize a series of 3-oxo-8,9;10,11-dianhydro-N-demethyl-clarithromycin derivatives and to evaluate their antiproliferative activities.Methods With clarithromycin as the starting material,target compounds were prepared by removing cladinose,protection of hydroxyl,oxidation,deprotection of hydroxyl,demethylation,and acylation.All compounds were evaluated for their antiproliferative activities against three human cancer cell lines(HT-1080,KB and SGC-7901)by the MTT assay.Results Ten novel bicyclic clarithromycin derivatives were synthesized and characterized by 13C-NMR and HRMS.Among them,12f and 12g showed the best antitumor activities.Conclusion The bicyclic clarithromycin derivatives have certain antitumor activity,which provides a new idea for the research of innovative antitumor drugs.
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