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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2007-10-1
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pubmed:abstractText |
The development of 2,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-ones as inhibitors of Chk1 kinase is described. Introduction of a fused ring at the C7/C8 positions of the pyrazoloquinolinone provided an increase in potency while guidance from overlapping inhibitor bound Chk1 X-ray crystal structures contributed to the discovery of a potent and solubilizing propyl amine moiety in compound 52 (Chk1 IC(50)=3.1 nM).
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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 |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ArringtonKenneth LKL,
pubmed-author:BeckStephen CSC,
pubmed-author:BrnardicEdward JEJ,
pubmed-author:BuserCarolyn ACA,
pubmed-author:DrakasBob ABA,
pubmed-author:DudkinVadim YVY,
pubmed-author:FraleyMark EME,
pubmed-author:GarbaccioRobert MRM,
pubmed-author:HamiltonKellyK,
pubmed-author:HardwickJamesJ,
pubmed-author:HartmanGeorge DGD,
pubmed-author:IkutaMariM,
pubmed-author:KreatsoulasConstantineC,
pubmed-author:KuoLawrence CLC,
pubmed-author:LobellRobert BRB,
pubmed-author:MaoXianzhiX,
pubmed-author:MunshiSanjeev KSK,
pubmed-author:RickertKeithK,
pubmed-author:Sepp-LorenzinoLauraL,
pubmed-author:SteenJustin TJT,
pubmed-author:StirdivantSteven MSM,
pubmed-author:TaoWeikangW,
pubmed-author:TasberEdward SES,
pubmed-author:WalshEileen SES,
pubmed-author:YanYouweiY
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pubmed:issnType |
Print
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pubmed:day |
1
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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 |
5989-94
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pubmed:dateRevised |
2011-11-2
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pubmed:meshHeading |
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pubmed:year |
2007
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pubmed:articleTitle |
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. edward_brnardic@merck.com
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pubmed:publicationType |
Journal Article
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