Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine- 7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 16, 2014, Pages 3928-3935

  Barlaam, Bernard ^a   Cosulich, Sabina ^a   Degorce, Sébastien ^a   Fitzek, Martina ^a   Giordanetto, Fabrizio ^b   Green, Stephen ^a   Inghardt, Tord ^b   Hennequin, Laurent ^a   Hancox, Urs ^a   Lambert Van Der Brempt, Christine ^a   Morgentin, Rémy ^a   Pass, Sarah ^a   Plé, Patrick ^a   Saleh, Twana ^a   Ward, Lara ^a  

^a ASTRAZENECA   (United Kingdom)

^b ASTRAZENECA R AND D   (Sweden)

Author keywords

PI3K inhibitor; PTEN deficient tumours; Rational design

Indexed keywords

9 (1 ANILINOETHYL) 2 MORPHOLINO 4 OXO PYRIDO[1,2 A]PYRIMIDINE 7 CARBOXAMIDE DERIVATIVE; AMIDE; ANTINEOPLASTIC AGENT; PHOSPHATASE; PHOSPHATIDYLINOSITOL 3 KINASE BETA INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE DELTA INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE BETA; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE DELTA; PROTEIN KINASE B; UNCLASSIFIED DRUG; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER INHIBITION; CELL ASSAY; DRUG DESIGN; DRUG SELECTIVITY; ENANTIOMER; ENZYME ASSAY; HECK REACTION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PROTEIN PHOSPHORYLATION; QUANTITATIVE STRUCTURE PROPERTY RELATION; RACEMIC MIXTURE; SAPONIFICATION; SCID MOUSE; SINGLE DRUG DOSE; STILLE REACTION; TUMOR MODEL; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL PROLIFERATION; CHEMICAL STRUCTURE; CHEMISTRY; DEFICIENCY; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG SCREENING; ENZYMOLOGY; METABOLISM; NEOPLASMS, EXPERIMENTAL; ORAL DRUG ADMINISTRATION; PATHOLOGY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; ANTINEOPLASTIC AGENTS; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; MICE; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN KINASE INHIBITORS; PTEN PHOSPHOHYDROLASE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84905919661     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.06.040     Document Type: Article

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