Source:http://linkedlifedata.com/resource/pubmed/id/20850977
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
21
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pubmed:dateCreated |
2010-10-18
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pubmed:abstractText |
Our previous studies demonstrated that two cytotoxic ?-nitrostyrene derivatives, 3,4-methylenedioxy-?-nitrostyrene (MNS) and 4-O-benzoyl-3-methoxy-?-nitrostyrene (BMNS) exhibit potent anti-platelet activities. In this study, a series of ?-nitrostyrenes were synthesized and subjected to anti-platelet aggregation assay and cytotoxicity assay. The mono- and di-substitutions on the B ring of BMNS tended to increase the anti-platelet activity and decrease the cytotoxic activity. Of these, compounds 19 and 24 exhibited the most potent inhibitory effects on thrombin- and collagen-induced platelet aggregation (IC(50)?0.7 ?M) without significant cytotoxicity on a human cancer cell line (up to 20 ?M). Further studies indicated that compounds 19 and 24 inhibited platelet aggregation via prevention of glycoprotein IIb/IIIa activation. The potent and novel effects of BMNS derivatives make them attractive candidates for the development of new anti-platelet agents.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7621-7
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pubmed:meshHeading |
pubmed-meshheading:20850977-Cell Line, Tumor,
pubmed-meshheading:20850977-Humans,
pubmed-meshheading:20850977-Integrin beta3,
pubmed-meshheading:20850977-Platelet Aggregation,
pubmed-meshheading:20850977-Platelet Aggregation Inhibitors,
pubmed-meshheading:20850977-Structure-Activity Relationship,
pubmed-meshheading:20850977-Styrenes
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pubmed:year |
2010
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pubmed:articleTitle |
The synthesis and biologic evaluation of anti-platelet and cytotoxic ?-nitrostyrenes.
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pubmed:affiliation |
Graduate Institute of Natural Products, Chang Gung University, Taoyuan 333, Taiwan. pewehs@mail.cgu.edu.tw
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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