The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

Xiang, Yibin; Hirth, Bradford; Asmussen, Gary; Biemann, Hans-Peter; Bishop, Kimberly A; Good, Andrew; Fitzgerald, Maria; Gladysheva, Tatiana; Jain, Annuradha; Jancsics, Katherine; Liu, Jinyu; Metz, Markus; Papoulis, Andrew; Skerlj, Renato; Stepp, J David; Wei, Ronnie R

Xiang, Yibin; Hirth, Bradford; Asmussen, Gary; Biemann, Hans-Peter; Bishop, Kimberly A; Good, Andrew; Fitzgerald, Maria; Gladysheva, Tatiana; Jain, Annuradha; Jancsics, Katherine; Liu, Jinyu; Metz, Markus; Papoulis, Andrew; Skerlj, Renato; Stepp, J David; Wei, Ronnie R.

Affiliation

Xiang Y; Department of Medicinal Chemistry, Drug and Biomaterial R&D, Genzyme Corp., 153 Second Avenue, Waltham, MA 02451, USA. yibin.xiang@genzyme.com

Bioorg Med Chem Lett ; 21(10): 3050-6, 2011 May 15.

Article in En | MEDLINE | ID: mdl-21507633

Subject(s)

Benzofurans/chemistry; Carboxylic Acids/pharmacology; Enzyme Activation/drug effects; Enzyme Inhibitors/pharmacology; Proto-Oncogene Proteins c-pim-1/antagonists & inhibitors; Animals; Carboxylic Acids/chemical synthesis; Carboxylic Acids/chemistry; Crystallography, X-Ray; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Humans; Inhibitory Concentration 50; Microsomes, Liver/drug effects; Microsomes, Liver/enzymology; Models, Molecular; Molecular Structure; Rats

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzofurans / Carboxylic Acids / Enzyme Activation / Enzyme Inhibitors / Proto-Oncogene Proteins c-pim-1 Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Document type: Article Affiliation country: United States

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