Source:http://linkedlifedata.com/resource/pubmed/id/17064909
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
|
pubmed:dateCreated |
2006-11-20
|
pubmed:abstractText |
Novel chalcones were found as potent inhibitors of interleukin (IL)-5. 1-(2-Benzyloxy-6-hydroxyphenyl)-3-(4-hydroxyphenyl)-2-propen-1-one (2b, 78.8% inhibition at 50microM, IC(50)=25.3microM) was initially identified as a potent inhibitor of IL-5. This shows the compatible activity with budesonide or sophoricoside. To identify structural requirements, 26 chalcones were prepared and their inhibitory activities were tested against IL-5. Among them, compound 4-[(E)-3-(2-cyclohexylmethoxy-6-hydroxyphenyl)-3-oxoprop-1-enyl]benzenesulfonamide (2w, 99.5% inhibition at 50microM, IC(50)=1.8microM) shows the most potent activity. The important structural requirements of these chalcone analogs exhibiting the inhibitory activity against IL-5 were recognized as the following. (1) The hydrophobic group such as benzyloxy or cyclohexylmethoxy at 6-position of A ring is necessary. (2) The existence of phenolic hydroxyl at 6-position of A ring is critical. (3) Propenone unit as alpha,beta-unsaturated ketone is essential. (4) Electron withdrawing groups with hydrogen acceptor property at 4-position of B ring enhance the activity and quantitative structure-activity relationship of 2 regarding these substituents was determined.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0968-0896
|
pubmed:author |
pubmed-author:BangSeong-CheolSC,
pubmed-author:ChoSoo-HyunSH,
pubmed-author:JuJung-HunJH,
pubmed-author:JungSang-HunSH,
pubmed-author:KimMi-KyeongMK,
pubmed-author:KimYoungsooY,
pubmed-author:LeeSeung-HoSH,
pubmed-author:RyuJae-ChunJC,
pubmed-author:ShinHye-RimHR,
pubmed-author:SongGyu-YongGY,
pubmed-author:YangHyun-MoHM
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
104-11
|
pubmed:meshHeading |
pubmed-meshheading:17064909-Animals,
pubmed-meshheading:17064909-B-Lymphocytes,
pubmed-meshheading:17064909-Cell Line,
pubmed-meshheading:17064909-Cell Proliferation,
pubmed-meshheading:17064909-Chalcones,
pubmed-meshheading:17064909-Drug Evaluation, Preclinical,
pubmed-meshheading:17064909-Interleukin-5,
pubmed-meshheading:17064909-Mice,
pubmed-meshheading:17064909-Molecular Structure,
pubmed-meshheading:17064909-Structure-Activity Relationship
|
pubmed:year |
2007
|
pubmed:articleTitle |
Structural requirement of chalcones for the inhibitory activity of interleukin-5.
|
pubmed:affiliation |
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|