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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2004-3-4
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pubmed:abstractText |
In our continued effort to identify selective MRP1 modulators, we have developed two novel templates, 3 and 4, through rational drug design by identifying the key pharmacophore interaction at the 7-position of the pyrrolopyrimidine template 1. Further synthesis and SAR work on these novel templates gave a number of potent MRP1 modulators with great selectivity against Pgp. Additional studies to reduce the CYP3A4 inhibition are also reported. Several compounds of these classes were subjected to in vivo xenograft studies and in vivo efficacies were demonstrated.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/CYP3A protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/CYP3A4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 CYP3A,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Doxorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Multidrug Resistance-Associated...,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BakerStewartS,
pubmed-author:BoyceAnthonyA,
pubmed-author:BroadbridgeJanJ,
pubmed-author:CharltonPeterP,
pubmed-author:ChuckowreeIrinaI,
pubmed-author:CocksSimonS,
pubmed-author:DepledgePaulP,
pubmed-author:FaintRichardR,
pubmed-author:FarmerHayleyH,
pubmed-author:FolkesAdrianA,
pubmed-author:FreathyCarolineC,
pubmed-author:HancoxTimothy CTC,
pubmed-author:HarrisonJohnJ,
pubmed-author:MillerWarrenW,
pubmed-author:MistryPrakashP,
pubmed-author:ScottJohnJ,
pubmed-author:SohalSukhjitS,
pubmed-author:ThompsonDeanneD,
pubmed-author:WanNan ChiNC,
pubmed-author:WangShoumingS,
pubmed-author:WilsonFrancisF
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pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1339-50
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:14998324-Animals,
pubmed-meshheading:14998324-Area Under Curve,
pubmed-meshheading:14998324-Biological Availability,
pubmed-meshheading:14998324-Cell Line, Tumor,
pubmed-meshheading:14998324-Combinatorial Chemistry Techniques,
pubmed-meshheading:14998324-Cytochrome P-450 CYP3A,
pubmed-meshheading:14998324-Cytochrome P-450 Enzyme System,
pubmed-meshheading:14998324-Doxorubicin,
pubmed-meshheading:14998324-Drug Resistance, Multiple,
pubmed-meshheading:14998324-Drug Synergism,
pubmed-meshheading:14998324-Female,
pubmed-meshheading:14998324-Half-Life,
pubmed-meshheading:14998324-Humans,
pubmed-meshheading:14998324-Mice,
pubmed-meshheading:14998324-Mice, Inbred BALB C,
pubmed-meshheading:14998324-Mice, Nude,
pubmed-meshheading:14998324-Models, Molecular,
pubmed-meshheading:14998324-Multidrug Resistance-Associated Proteins,
pubmed-meshheading:14998324-P-Glycoprotein,
pubmed-meshheading:14998324-Pyrimidines,
pubmed-meshheading:14998324-Pyrroles,
pubmed-meshheading:14998324-Structure-Activity Relationship,
pubmed-meshheading:14998324-Xenograft Model Antitumor Assays
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pubmed:year |
2004
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pubmed:articleTitle |
Design and synthesis of new templates derived from pyrrolopyrimidine as selective multidrug-resistance-associated protein inhibitors in multidrug resistance.
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pubmed:affiliation |
Department of Medicinal Chemistry, Department of Pharmacology, Analytical Department, Xenova Ltd., 957 Buckingham Avenue, Slough, Berkshire SL1 4NL,UK. swang@trigen.co.uk
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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