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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2007-3-13
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pubmed:abstractText |
A new P1' group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1' group. Incorporation of this 4-(2-methylquinolin-4-ylmethyl)phenyl group onto different beta-aminohydroxamic acid cores provided compound 18, which demonstrated potent porcine TACE (p-TACE) and human whole blood activity, excellent PK properties, and good selectivity against a variety of MMPs.
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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 |
Apr
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ChenXiao-TaoXT,
pubmed-author:ChristDavid DDD,
pubmed-author:CorbettRonald LRL,
pubmed-author:CovingtonMaryanne BMB,
pubmed-author:DeciccoCarl PCP,
pubmed-author:DuanJames J-WJJ,
pubmed-author:GhavimiBahmanB,
pubmed-author:HartmanKarl DKD,
pubmed-author:LiuRui-QinRQ,
pubmed-author:NewtonRobert CRC,
pubmed-author:QianMingxinM,
pubmed-author:RibadeneiraMaria DMD,
pubmed-author:TrzaskosJames MJM,
pubmed-author:VaddiKrishna GKG,
pubmed-author:XueChu-BiaoCB
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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 |
1865-70
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pubmed:meshHeading |
pubmed-meshheading:17276676-ADAM Proteins,
pubmed-meshheading:17276676-Animals,
pubmed-meshheading:17276676-Chemistry, Pharmaceutical,
pubmed-meshheading:17276676-Dogs,
pubmed-meshheading:17276676-Drug Design,
pubmed-meshheading:17276676-Enzyme Inhibitors,
pubmed-meshheading:17276676-Humans,
pubmed-meshheading:17276676-Hydroxamic Acids,
pubmed-meshheading:17276676-Inhibitory Concentration 50,
pubmed-meshheading:17276676-Models, Chemical,
pubmed-meshheading:17276676-Molecular Conformation,
pubmed-meshheading:17276676-Oxygen,
pubmed-meshheading:17276676-Rats,
pubmed-meshheading:17276676-Structure-Activity Relationship,
pubmed-meshheading:17276676-Swine
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pubmed:year |
2007
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pubmed:articleTitle |
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
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pubmed:affiliation |
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. xiao-tao.chen@bms.com
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pubmed:publicationType |
Journal Article
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