Source:http://linkedlifedata.com/resource/pubmed/id/21295889
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2011-3-4
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pubmed:abstractText |
By using human scavenger receptor CD36 as the target, twenty-five N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their antagonistic activities for CD36-oxidatively low density lipoprotein (oxLDL) binding. The primary analysis of structure-activity relationship (SAR) indicated a methoxyl at the 7-position and a hydroxyl at the 6- or 8-position could afford good activities. Among these analogs, compounds 7e and 7t showed the potential CD36 antagonistic activities with IC(50) values of 0.2 and 0.8 ?g/mL, respectively. Furthermore, both of them could effectively inhibit oxLDL uptake in insect Sf9 cells overexpressing human CD36, and thus have been selected for further investigation. We consider N-(2-arylethyl) isoquinoline analogs to be a family of novel CD36 antagonists.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antigens, CD36,
http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Lipoproteins, LDL,
http://linkedlifedata.com/resource/pubmed/chemical/isoquinoline,
http://linkedlifedata.com/resource/pubmed/chemical/oxidized low density lipoprotein
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1768-3254
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pubmed:author |
pubmed-author:DiemEE,
pubmed-author:HuntH LHL,
pubmed-author:JiangJian-DongJD,
pubmed-author:LiYang-BiaoYB,
pubmed-author:LiYing-HongYH,
pubmed-author:ShanYong-QiangYQ,
pubmed-author:SiShu-YiSY,
pubmed-author:SongDan-QingDQ,
pubmed-author:WangLiL,
pubmed-author:WangYan-XiangYX,
pubmed-author:XuYan-NiYN
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1066-73
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pubmed:meshHeading |
pubmed-meshheading:21295889-Animals,
pubmed-meshheading:21295889-Antigens, CD36,
pubmed-meshheading:21295889-Cell Line,
pubmed-meshheading:21295889-Drug Design,
pubmed-meshheading:21295889-Humans,
pubmed-meshheading:21295889-Isoquinolines,
pubmed-meshheading:21295889-Lipoproteins, LDL,
pubmed-meshheading:21295889-Microscopy, Fluorescence,
pubmed-meshheading:21295889-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists.
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pubmed:affiliation |
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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