Chen Jiaojiao, Lu Min, Jing Yongkui, Dong Jinhua
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Bioorg Med Chem. 2006 Oct 1;14(19):6539-47. doi: 10.1016/j.bmc.2006.06.013. Epub 2006 Jun 27.
Thirty-one novel derivatives of carvone, carveol, and limonene were designed and synthesized using L-carvone as a starting material via chlorination, nucleophilic substitution, and reduction. The structures of these derivatives were characterized by MS and 1H NMR. The antiproliferative effect was evaluated in human prostate cancer LNCaP cells. L-carvone, L-carveol, and L-limonene were weak cell growth inhibitors and introduction of 4-(2-methoxyphenyl)piperazine to carvone, carveol or limonene significantly increased their antiproliferative effect. The antiproliferative effect was correlated with ERK activation and p21(waf1) induction.
以L-香芹酮为起始原料，通过氯化、亲核取代和还原反应，设计并合成了31种香芹酮、香芹醇和柠檬烯的新型衍生物。这些衍生物的结构通过质谱（MS）和核磁共振氢谱（1H NMR）进行了表征。在人前列腺癌LNCaP细胞中评估了它们的抗增殖作用。L-香芹酮、L-香芹醇和L-柠檬烯是较弱的细胞生长抑制剂，而将4-(2-甲氧基苯基)哌嗪引入香芹酮、香芹醇或柠檬烯中可显著增强它们的抗增殖作用。抗增殖作用与细胞外信号调节激酶（ERK）激活和p21（waf1）诱导相关。
