Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives

Molecules

Zi Hui²  Meihui Zhang²  Lin Cong¹  Mingyu Xia¹ 

[1] School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mail:;Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mails:

关键词: perillyl alcohol;    perillyl alcohol derivative;    amino-modification;    antiproliferation;    apoptosis induction;   

DOI  :  10.3390/molecules19056671

来源: mdpi

【 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 IC₅₀s below 100 μM. It was demonstrated that the antiproliferative effect of VI₅ was mediated through the induction of apoptosis in A549 cells.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.