|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0011953,
umls-concept:C0144544,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243077,
umls-concept:C0442027,
umls-concept:C0723595,
umls-concept:C0796679,
umls-concept:C0935763,
umls-concept:C1412186,
umls-concept:C1527415
|
|
pubmed:issue |
10
|
|
pubmed:dateCreated |
2011-5-2
|
|
pubmed:abstractText |
TNF-? converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
May
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:ChenShiyingS,
pubmed-author:DaiChaoyangC,
pubmed-author:GirijavallabhanVinay MVM,
pubmed-author:GuoZhuyanZ,
pubmed-author:KozlowskiJoseph AJA,
pubmed-author:LaveyBrian JBJ,
pubmed-author:LiDansuD,
pubmed-author:LundellDaniel JDJ,
pubmed-author:NiuXiaodaX,
pubmed-author:OrthPeterP,
pubmed-author:PiwinskiJohn JJJ,
pubmed-author:Popovici-MullerJanetaJ,
pubmed-author:RizviRaziaR,
pubmed-author:RosnerKristin EKE,
pubmed-author:ShankarBandarpalle BBB,
pubmed-author:ShihNeng-YangNY,
pubmed-author:SiddiquiM ArshadMA,
pubmed-author:StricklandCorey OCO,
pubmed-author:SunJingJ,
pubmed-author:WongMichael K CMK,
pubmed-author:ZhaoLianyunL
|
|
pubmed:copyrightInfo |
Copyright © 2011. Published by Elsevier Ltd.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
15
|
|
pubmed:volume |
21
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
3172-6
|
|
pubmed:meshHeading |
|
|
pubmed:year |
2011
|
|
pubmed:articleTitle |
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
|
|
pubmed:affiliation |
Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, USA. chaoyang.dai@merck.com
|
|
pubmed:publicationType |
Journal Article
|
