Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives

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...

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Main Authors:	Zi Hui, Meihui Zhang, Lin Cong, Mingyu Xia, Jinhua Dong
Format:	Article
Language:	English
Published:	MDPI AG 2014-05-01
Series:	Molecules
Subjects:	perillyl alcohol perillyl alcohol derivative amino-modification antiproliferation apoptosis induction
Online Access:	http://www.mdpi.com/1420-3049/19/5/6671

id	doaj-4e673eebaf4b4dacbe1f249596df9cae
record_format	Article
spelling	doaj-4e673eebaf4b4dacbe1f249596df9cae2020-11-24T20:56:58ZengMDPI AGMolecules1420-30492014-05-011956671668210.3390/molecules19056671molecules19056671Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol DerivativesZi Hui0Meihui Zhang1Lin Cong2Mingyu Xia3Jinhua Dong4Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaSchool of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, ChinaSchool of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, ChinaKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, ChinaTwo 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.http://www.mdpi.com/1420-3049/19/5/6671perillyl alcoholperillyl alcohol derivativeamino-modificationantiproliferationapoptosis induction
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Zi Hui Meihui Zhang Lin Cong Mingyu Xia Jinhua Dong
spellingShingle	Zi Hui Meihui Zhang Lin Cong Mingyu Xia Jinhua Dong Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives Molecules perillyl alcohol perillyl alcohol derivative amino-modification antiproliferation apoptosis induction
author_facet	Zi Hui Meihui Zhang Lin Cong Mingyu Xia Jinhua Dong
author_sort	Zi Hui
title	Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives
title_short	Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives
title_full	Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives
title_fullStr	Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives
title_full_unstemmed	Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives
title_sort	synthesis and antiproliferative effects of amino-modified perillyl alcohol derivatives
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2014-05-01
description	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.
topic	perillyl alcohol perillyl alcohol derivative amino-modification antiproliferation apoptosis induction
url	http://www.mdpi.com/1420-3049/19/5/6671
work_keys_str_mv	AT zihui synthesisandantiproliferativeeffectsofaminomodifiedperillylalcoholderivatives AT meihuizhang synthesisandantiproliferativeeffectsofaminomodifiedperillylalcoholderivatives AT lincong synthesisandantiproliferativeeffectsofaminomodifiedperillylalcoholderivatives AT mingyuxia synthesisandantiproliferativeeffectsofaminomodifiedperillylalcoholderivatives AT jinhuadong synthesisandantiproliferativeeffectsofaminomodifiedperillylalcoholderivatives
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Synthesis and Antiproliferative Effects of Amino-Modified Perillyl Alcohol Derivatives

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