Background：Several studies have shown excellent antitumor activity of erucin, but there are
few studies on its analogues. The aim of the study involves the synthesis and the antitumor activities of
novel erucin analogues. Ten novel erucin analogues were synthesized and evaluated for their efficacy
as antitumor agents.
Methods: Ten novel erucin analogues were synthesized by using 1, 4-dibromobutane and potassium
phthalimide as starting materials, and the antitumor activities in vitro was screened against breast cancer
cells (MCF-7), cervical cancer cells (HeLa-229) and lung cancer cells (A549).
Results: The structures of these novel compounds were confirmed by 1H NMR, 13C NMR and elemental
analysis. The preliminary bioassay results demonstrated that all of the tested compounds showed
potent antitumor activities. Among these compounds, compound 6b showed the best inhibitory effect
against MCF-7 with IC50 value of 0.46 µM and A549 with IC50 value of 0.44 µM. Compound 6f also
displayed the best inhibitory effect against HeLa-229 with IC50 value of 0.32 µM.
Conclusion: Synthesis and screening of antitumor activities were performed for a novel series of
erucin analogues. All of the synthetic compounds showed potent antitumor activities against breast
cancer cells (MCF-7), cervical cancer cells (HeLa-229) and lung cancer cells (A549). Compounds 6b
and 6f were found to be the most active against most of the tested cancer cells.