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

Bioorganic & Medicinal Chemistry
Liying XuJin-Hua Dong

Abstract

Fourteen beta-elemene derivatives containing a piperazine, a morpholine, a tetrahydropyrrole, a thiophenylethylamine, or a cyclohexamine group were synthesized. The structures of these beta-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 beta-elemene. Among these derivatives, 13,14-bis(cis-3,5-dimethyl-1-piperazinyl)-beta-elemene (IIi), 13,14-bis[2-(2-thiophenyl)ethylamino]-beta-elemene (IIm), and 13,14-bis(cyclohexamino)-beta-elemene (IIn) were the most potent agents. IIi, IIm, and IIn inhibited K562 cell growth with an IG50 below 5 microM that was correlated with mTOR activity inhibition.

References

Jan 12, 2000·Anti-cancer Drugs·A Sandler, A T van Oosterom
Aug 13, 2005·Anti-cancer Drugs·Daniel Morgensztern, Howard L McLeod

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Citations

May 24, 2012·International Journal of Nanomedicine·Feng ShiNian-Ping Feng
May 28, 2013·Evidence-based Complementary and Alternative Medicine : ECAM·Bing YanZhifeng Qin
Jul 24, 2012·Journal of Ethnopharmacology·Jin-Jian LuYi-Tao Wang
May 27, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Zi HuiJinhua Dong
Apr 20, 2012·The Cochrane Database of Systematic Reviews·Rui DongGuan J Liu
Apr 11, 2009·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Yanhong SunYu-Mei Shen
Jul 13, 2013·Molecular Nutrition & Food Research·Bharat B AggarwalSubash C Gupta
Jun 17, 2020·Royal Society Open Science·Xingrui HeTian Xie
Apr 4, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ziqiang BaiTian Xie

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