Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.

Pecchi, Sabina; Ni, Zhi-Jie; Han, Wooseok; Smith, Aaron; Lan, Jiong; Burger, Matthew; Merritt, Hanne; Wiesmann, Marion; Chan, John; Kaufman, Susan; Knapp, Mark S; Janssen, Johanna; Huh, Kay; Voliva, Charles F

Pecchi, Sabina; Ni, Zhi-Jie; Han, Wooseok; Smith, Aaron; Lan, Jiong; Burger, Matthew; Merritt, Hanne; Wiesmann, Marion; Chan, John; Kaufman, Susan; Knapp, Mark S; Janssen, Johanna; Huh, Kay; Voliva, Charles F.

Affiliation

Pecchi S; Global Discovery Chemistry/Oncology and Exploratory Chemistry, Novartis Institutes for Biomedical Research, Emeryville, CA, USA.

Bioorg Med Chem Lett ; 23(16): 4652-6, 2013 Aug 15.

Article in En | MEDLINE | ID: mdl-23820386

Subject(s)

Azo Compounds/chemical synthesis; Phosphoinositide-3 Kinase Inhibitors; Pyridines/chemical synthesis; Pyridines/pharmacology; Azo Compounds/chemistry; Azo Compounds/pharmacology; Benzothiazoles/chemistry; Benzothiazoles/pharmacology; Cell Line, Tumor; Enzyme Activation/drug effects; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Female; Humans; Imides/chemical synthesis; Imides/chemistry; Imides/pharmacology; Inhibitory Concentration 50; Models, Molecular; Pyridines/chemistry; Solubility; Structure-Activity Relationship

Key words

Cancer; Imidazopyridine; Lipid kinase; PI3 kinase inhibitor; Scaffold morphing; Structure-guided drug design

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Azo Compounds / Phosphoinositide-3 Kinase Inhibitors Limits: Female / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Document type: Article Affiliation country: United States Country of publication: United kingdom

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