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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Xu L,Tao S,Wang X,Yu Z,Wang M,Chen D,Jing Y,Dong J

doi

10.1016/j.bmc.2006.03.041

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

5351-6

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00253-7

journal_volume

14

pub_type

杂志文章

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