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rdf:type |
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lifeskim:mentions |
umls-concept:C0020314,
umls-concept:C0068935,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243077,
umls-concept:C0442027,
umls-concept:C0529196,
umls-concept:C0679622,
umls-concept:C0935763,
umls-concept:C1412186,
umls-concept:C1527415,
umls-concept:C1705542,
umls-concept:C1880355,
umls-concept:C2003941
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pubmed:issue |
4
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pubmed:dateCreated |
2008-2-18
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pubmed:abstractText |
Two novel oxaspiro[4.4]nonane beta-benzamido hydroxamic scaffolds have been synthesized in enantio- and diasteriomerically pure form. These templates proved to be exceptional platforms that have led to the discovery of potent inhibitors of TACE that are active in a cellular assay measuring suppression of LPS-induced TNF-alpha. Furthermore, these inhibitors are selective against related MMPs, demonstrate permeability in a Caco-2 assay, and display good oral bioavailability.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AsakawaNaoyukiN,
pubmed-author:ChristDavid DDD,
pubmed-author:CovingtonMaryanne BMB,
pubmed-author:DuanJames J-WJJ,
pubmed-author:GalyaLaurineL,
pubmed-author:LiuRui-QinRQ,
pubmed-author:MarshallWillW,
pubmed-author:NewtonRobert CRC,
pubmed-author:OttGregory RGR,
pubmed-author:QianMingxinM,
pubmed-author:ScholzThomasT,
pubmed-author:TrzaskosJames MJM,
pubmed-author:VaddiKrishnaK
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
|
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1288-92
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pubmed:meshHeading |
pubmed-meshheading:18234496-ADAM Proteins,
pubmed-meshheading:18234496-Administration, Oral,
pubmed-meshheading:18234496-Alkanes,
pubmed-meshheading:18234496-Animals,
pubmed-meshheading:18234496-Biological Availability,
pubmed-meshheading:18234496-Caco-2 Cells,
pubmed-meshheading:18234496-Humans,
pubmed-meshheading:18234496-Hydroxamic Acids,
pubmed-meshheading:18234496-Matrix Metalloproteinases,
pubmed-meshheading:18234496-Models, Molecular,
pubmed-meshheading:18234496-Protease Inhibitors,
pubmed-meshheading:18234496-Rats,
pubmed-meshheading:18234496-Rats, Sprague-Dawley,
pubmed-meshheading:18234496-Spiro Compounds
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pubmed:year |
2008
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pubmed:articleTitle |
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
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pubmed:affiliation |
Departments of Discovery Chemistry and Discovery Biology, Bristol-Myers Squibb Research and Development, Rte 206 and Province Line Road, Princeton, NJ 08543, USA.
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pubmed:publicationType |
Journal Article
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