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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2003-12-30
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pubmed:abstractText |
Modifications to the basic side-chain of early lead structures of the indolyl quinolinone class of KDR kinase inhibitors resulted in improved pharmacokinetic and ancillary profiles. Specifically, compounds bearing 5-amido- and 5-sulphonamido-indolyl substituents exhibited lower plasma clearance and weaker binding affinity for the I(Kr) potassium channel hERG.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ArringtonKenneth LKL,
pubmed-author:BuserCarolyn ACA,
pubmed-author:CieckoPatrice APA,
pubmed-author:CollKathleen EKE,
pubmed-author:FernandesChristineC,
pubmed-author:FraleyMark EME,
pubmed-author:HartmanGeorge DGD,
pubmed-author:HoffmanWilliam FWF,
pubmed-author:LynchJoseph JJJ,
pubmed-author:McFallRosemary CRC,
pubmed-author:RickertKeithK,
pubmed-author:SinghRomiR,
pubmed-author:SmithSheriS,
pubmed-author:ThomasKenneth AKA,
pubmed-author:WongBradley KBK
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pubmed:issnType |
Print
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pubmed:day |
19
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
351-5
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:14698157-Animals,
pubmed-meshheading:14698157-Cation Transport Proteins,
pubmed-meshheading:14698157-Cell Line,
pubmed-meshheading:14698157-Dogs,
pubmed-meshheading:14698157-Enzyme Inhibitors,
pubmed-meshheading:14698157-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:14698157-Humans,
pubmed-meshheading:14698157-Microsomes, Liver,
pubmed-meshheading:14698157-Potassium Channels,
pubmed-meshheading:14698157-Potassium Channels, Voltage-Gated,
pubmed-meshheading:14698157-Protein Binding,
pubmed-meshheading:14698157-Quinolones,
pubmed-meshheading:14698157-Rats,
pubmed-meshheading:14698157-Vascular Endothelial Growth Factor Receptor-2
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pubmed:year |
2004
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pubmed:articleTitle |
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. mark_fraley@merck.com
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pubmed:publicationType |
Journal Article
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