Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin- 5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 6, 2012, Pages 2230-2234

  Lin, Hong ^a   Erhard, Karl ^a   Hardwicke, Mary Ann ^a   Luengo, Juan I ^a   MacK, James F ^a   McSurdy Freed, Jeanelle ^a   Plant, Ramona ^a   Raha, Kaushik ^a   Rominger, Cynthia M ^a   Sanchez, Robert M ^a   Schaber, Michael D ^a   Schulz, Mark J ^a   Spengler, Michael D ^a   Tedesco, Rosanna ^a   Xie, Ren ^a   Zeng, Jin J ^a   Rivero, Ralph A ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Homology model; Phosphatidylinositol 3 kinase; PI3K beta inhibitor; PTEN null; Structure activity relationship

Indexed keywords

9 (1 ANILINOETHYL) 7 METHYL 2 MORPHOLINOPYRIDO[1,2 A]PYRIMIDIN 4 ONE; ANTINEOPLASTIC AGENT; IMIDAZO[1,2 A]PYRIMIDIN 5(1H) ONE DERIVATIVE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BREAST CANCER; CANCER INHIBITION; CHIRALITY; CONTROLLED STUDY; DRUG DESIGN; DRUG SYNTHESIS; ENANTIOMER; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; BINDING SITES; BREAST NEOPLASMS; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; GENE DELETION; HUMANS; IMIDAZOLES; ISOENZYMES; KINETICS; MODELS, MOLECULAR; PHOSPHATIDYLINOSITOL 3-KINASE; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PTEN PHOSPHOHYDROLASE; PYRIMIDINONES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84862800391     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.092     Document Type: Article

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