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4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.
Han, Qiang; Pabba, Praveen K; Barbosa, Joseph; Mabon, Ross; Healy, Jason P; Gardyan, Michael W; Terranova, Kristen M; Brommage, Robert; Thompson, Andrea Y; Schmidt, James M; Wilson, Alan G E; Xu, Xiaolian; Tarver, James E; Carson, Kenneth G.
Affiliation
  • Han Q; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Pabba PK; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Barbosa J; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Mabon R; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Healy JP; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Gardyan MW; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Terranova KM; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Brommage R; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
  • Thompson AY; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
  • Schmidt JM; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
  • Wilson AG; Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
  • Xu X; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • Tarver JE; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States. Electronic address: james.tarver2@gmail.com.
  • Carson KG; Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
Bioorg Med Chem Lett ; 26(4): 1184-7, 2016 Feb 15.
Article in En | MEDLINE | ID: mdl-26821819
ABSTRACT
A group of small molecule thienochromenes inhibitors of Notum Pectinacetylesterase are described. We developed SAR on three series based on carbon, oxygen and sulfur replacement of the 5-position. In each series, highly potent Notum Pectinacetylesterase inhibitors were identified.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzopyrans / Enzyme Inhibitors / Esterases Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Benzopyrans / Enzyme Inhibitors / Esterases Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article Affiliation country: United States