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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2007-9-18
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pubmed:abstractText |
Observations from two structurally related series of KSP inhibitors led to the proposal and discovery of dihydropyrazolobenzoxazines that possess ideal properties for cancer drug development. The synthesis and characterization of this class of inhibitors along with relevant pharmacokinetic and in vivo data are presented. The synthesis is highlighted by a key [3+2] cycloaddition to form the pyrazolobenzoxazine core followed by diastereospecific installation of a quaternary center.
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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 |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BergmanJeffJ,
pubmed-author:BuserCarolyn ACA,
pubmed-author:ColemanPaul JPJ,
pubmed-author:DavideJoseph PJP,
pubmed-author:DiehlRonald ERE,
pubmed-author:Fernandez-MetzlerCarmenC,
pubmed-author:FraleyMark EME,
pubmed-author:GarbaccioRobert MRM,
pubmed-author:HamiltonKellyK,
pubmed-author:HartmanGeorge DGD,
pubmed-author:HuberHans EHE,
pubmed-author:KohlNancy ENE,
pubmed-author:KuoLawrence CLC,
pubmed-author:LiChunzeC,
pubmed-author:LobellRobert BRB,
pubmed-author:MahanElizabeth AEA,
pubmed-author:NeilsonLou AnneLA,
pubmed-author:OlsonChristyC,
pubmed-author:PrueksaritanontThomayantT,
pubmed-author:RickertKeithK,
pubmed-author:SalataJoseph JJJ,
pubmed-author:SlaughterDonald EDE,
pubmed-author:SouthVicki JVJ,
pubmed-author:TaoWeikangW,
pubmed-author:TasberEdward SES,
pubmed-author:TorrentMaricelM,
pubmed-author:WalshEileen SES,
pubmed-author:YanYouweiY
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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 |
5671-6
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pubmed:meshHeading |
pubmed-meshheading:17804233-Animals,
pubmed-meshheading:17804233-Benzoxazines,
pubmed-meshheading:17804233-Cell Line,
pubmed-meshheading:17804233-Dogs,
pubmed-meshheading:17804233-Drug Design,
pubmed-meshheading:17804233-Humans,
pubmed-meshheading:17804233-Hydrogen,
pubmed-meshheading:17804233-Kinesin,
pubmed-meshheading:17804233-Mitosis,
pubmed-meshheading:17804233-Molecular Structure,
pubmed-meshheading:17804233-Pyrazoles,
pubmed-meshheading:17804233-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. robert_garbaccio@merck.com
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pubmed:publicationType |
Journal Article
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