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 inc...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2006-08, Vol.14 (15), p.5351-5356
Hauptverfasser: Xu, Liying, Tao, Shujuan, Wang, Xianming, Yu, Zhiying, Wang, Minwei, Chen, Duo, Jing, Yongkui, Dong, Jinhua
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Sprache:eng
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Zusammenfassung: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 IG 50 below 5 μM that was correlated with mTOR activity inhibition.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.03.041