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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2007-4-30
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pubmed:abstractText |
A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.
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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 |
May
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AlbrechtBrian KBK,
pubmed-author:BellonSteveS,
pubmed-author:CaenepeelSeanS,
pubmed-author:CeeVictor JVJ,
pubmed-author:ChaffeeStuart CSC,
pubmed-author:EmeryMauriceM,
pubmed-author:FretlandJenneJ,
pubmed-author:GallantPaulP,
pubmed-author:Geuns-MeyerStephanie DSD,
pubmed-author:GuYanY,
pubmed-author:HodousBrian LBL,
pubmed-author:HughesPaul EPE,
pubmed-author:JohnsonRebecca ERE,
pubmed-author:KimJoseph LJL,
pubmed-author:LongAlexander MAM,
pubmed-author:MorrisonMichaelM,
pubmed-author:OlivieriPhilip RPR,
pubmed-author:PatelVinod FVF,
pubmed-author:PolverinoAnthonyA,
pubmed-author:RosePaulP,
pubmed-author:WangLingL,
pubmed-author:ZhaoHuilinH
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2886-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17350837-Animals,
pubmed-meshheading:17350837-Crystallography, X-Ray,
pubmed-meshheading:17350837-Drug Design,
pubmed-meshheading:17350837-Male,
pubmed-meshheading:17350837-Models, Molecular,
pubmed-meshheading:17350837-Molecular Structure,
pubmed-meshheading:17350837-Rats,
pubmed-meshheading:17350837-Rats, Sprague-Dawley,
pubmed-meshheading:17350837-Receptor, TIE-2,
pubmed-meshheading:17350837-Structure-Activity Relationship,
pubmed-meshheading:17350837-Triazines
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. bhodous@amgen.com
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pubmed:publicationType |
Journal Article
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