The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor
Hynes, John Wu, Hong Pitt, Sidney Shen, Ding Ren Zhang, Rosemary F. Schieven, Gary L. Gillooly, Kathleen M. Shuster, David J. Taylor, Tracy L. Yang, XiaoXia
Hynes, John
Wu, Hong
Pitt, Sidney
Shen, Ding Ren
Zhang, Rosemary F.
Schieven, Gary L.
Gillooly, Kathleen M.
Shuster, David J.
Taylor, Tracy L.
Yang, XiaoXia
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Authors
Hynes, John
Wu, Hong
Pitt, Sidney
Shen, Ding Ren
Zhang, Rosemary F.
Schieven, Gary L.
Gillooly, Kathleen M.
Shuster, David J.
Taylor, Tracy L.
Yang, XiaoXia
McIntyre, Kim W.
McKinnon, Murray
Zhang, Hongjian
Marathe, Punit H.
Doweyko, Arthur M.
Kish, Kevin
Kiefer, Susan E.
Sack, John S.
Newitt, John A.
Barrish, Joel C.
Dodd, John H.
Leftheris, Katerina
Wu, Hong
Pitt, Sidney
Shen, Ding Ren
Zhang, Rosemary F.
Schieven, Gary L.
Gillooly, Kathleen M.
Shuster, David J.
Taylor, Tracy L.
Yang, XiaoXia
McIntyre, Kim W.
McKinnon, Murray
Zhang, Hongjian
Marathe, Punit H.
Doweyko, Arthur M.
Kish, Kevin
Kiefer, Susan E.
Sack, John S.
Newitt, John A.
Barrish, Joel C.
Dodd, John H.
Leftheris, Katerina
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Faculty Advisor
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UMass Chan Affiliations
Document Type
Journal Article
Publication Date
2008-03-04
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Abstract
A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.
Source
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. Epub 2008 Feb 16. Link to article on publisher's site
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DOI
10.1016/j.bmcl.2008.02.031
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PubMed ID
18313298