Abstract: A series of triazole derivatives were designed and synthesized based on a natural product cembrane separated from Croton laevigatus Vahl which showed potential antitumor activity against HeLa cells. Twelve novel compounds were synthesized and their structures were characterized by ¹H NMR, ¹³C NMR and HRMS. Their cytotoxicities in vitro were evaluated for HeLa, K562 and K562/A02 cells by MTT assay. The results showed that some cembrane derivatives possessed antitumor activities. Substituted triazole connected to cembrane derivatives exhibited potent activity toward drug-resistant K562/A02 cells.