The synthesis and anti-proliferative effects of β-elemene derivatives with mTOR inhibition activity

Fourteen β-elemene derivatives containing a piperazine, a morpholine, a tetrahydropyrrole, a thiophenylethylamine, or a cyclohexamine group were synthesized. The structures of these β-elemene derivatives were characterized with IR, 1H NMR, MS, and elemental analyses. All these derivatives had an increased anti-proliferative activity in human cervix epitheloid carcinoma HeLa, gastric carcinoma SGC-7901, and leukemia K562 cells comparing with that of β-elemene. Among these derivatives, 13,14-bis(cis-3,5-dimethyl-1-piperazinyl)-β-elemene (IIi), 13,14-bis[2-(2-thiophenyl)ethylamino]-β-elemene (IIm), and 13,14-bis(cyclohexamino)-β-elemene (IIn) were the most potent agents. IIi, IIm, and IIn inhibited K562 cell growth with an IG50 below 5 μM that was correlated with mTOR activity inhibition.

Figure optionsDownload as PowerPoint slide