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Molecules 2014, 19(5), 6671-6682; doi:10.3390/molecules19056671

Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives

1
Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
2
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
*
Authors to whom correspondence should be addressed.
Received: 18 April 2014 / Revised: 6 May 2014 / Accepted: 16 May 2014 / Published: 22 May 2014
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Abstract

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. View Full-Text
Keywords: perillyl alcohol; perillyl alcohol derivative; amino-modification; antiproliferation; apoptosis induction perillyl alcohol; perillyl alcohol derivative; amino-modification; antiproliferation; apoptosis induction
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Hui, Z.; Zhang, M.; Cong, L.; Xia, M.; Dong, J. Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives. Molecules 2014, 19, 6671-6682.

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