Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives

被引:15
作者
Hui, Zi [1 ]
Zhang, Meihui [1 ]
Cong, Lin [2 ]
Xia, Mingyu [2 ]
Dong, Jinhua [1 ]
机构
[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China
[2] Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Shenyang 110016, Peoples R China
关键词
perillyl alcohol; perillyl alcohol derivative; amino-modification; antiproliferation; apoptosis induction; PHASE-II TRIAL; PROSTATE-CANCER; INHIBITION; CELLS; LIMONENE; ISOPRENYLATION; MONOTERPENE; METABOLITES; ACTIVATION; DEATH;
D O I
10.3390/molecules19056671
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Two series of amino-modified derivatives of (S)-perillyl alcohol were designed and synthesized using (S)-perillaldehyde as the starting material. These derivatives showed increased antiproliferative activity in human lung cancer A549 cells, human melanoma A375-S2 cells and human fibrosarcoma HT-1080 cells comparing with that of (S)-perillyl alcohol. Among these derivatives, compounds VI5 and VI7 were the most potent agents, with the IC(50)s below 100 mu M. It was demonstrated that the antiproliferative effect of VI5 was mediated through the induction of apoptosis in A549 cells.
引用
收藏
页码:6671 / 6682
页数:12
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