Xu Liying, Tao Shujuan, Wang Xianming, Yu Zhiying, Wang Minwei, Chen Duo, Jing Yongkui, Dong Jinhua
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Bioorg Med Chem. 2006 Aug 1;14(15):5351-6. doi: 10.1016/j.bmc.2006.03.041. Epub 2006 Apr 17.
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.
合成了14种含有哌嗪、吗啉、四氢吡咯、苯乙硫胺或环己胺基团的β-榄香烯衍生物。通过红外光谱、核磁共振氢谱、质谱和元素分析对这些β-榄香烯衍生物的结构进行了表征。与β-榄香烯相比，所有这些衍生物在人宫颈上皮样癌HeLa、胃癌SGC-7901和白血病K562细胞中的抗增殖活性均有所增强。在这些衍生物中，13,14-双（顺式-3,5-二甲基-1-哌嗪基）-β-榄香烯（IIi）、13,14-双[2-（2-噻吩基）乙氨基]-β-榄香烯（IIm）和13,14-双（环己氨基）-β-榄香烯（IIn）是最有效的药物。IIi、IIm和IIn抑制K562细胞生长的IG50低于5微摩尔，这与mTOR活性抑制相关。
