Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivity

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 17, 2013, Pages 4953-4959

  Safina, Brian S ^a   Sweeney, Zachary K ^a   Li, Jun ^a   Chan, Bryan K ^a   Bisconte, Angelina ^a   Carrera, Diane ^a   Castanedo, Georgette ^a   Flagella, Michael ^a   Heald, Robert ^b   Lewis, Cristina ^a   Murray, Jeremy M ^a   Nonomiya, Jim ^a   Pang, Jodie ^a   Price, Steve ^b   Reif, Karin ^a   Salphati, Laurent ^a   Seward, Eileen M ^b   Wei, Binqing ^a   Sutherlin, Daniel P ^a  

^a GENENTECH INC   (United States)

^b Argenta Discovery Ltd   (United Kingdom)

Author keywords

B cell inhibition; Genotox; HCA; MNT; PI3K ; PI3K isoform selectivity

Indexed keywords

CARBENE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR;

ARTICLE; GENOTOXICITY; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MECHANICAL TORSION; MICRONUCLEUS; NONHUMAN;

B-CELL INHIBITION; GENOTOX; HCA; MNT; PI3K ISOFORM SELECTIVITY; PI3K Δ;

ANIMALS; CELL LINE; CYCLIC S-OXIDES; DOGS; HUMANS; MOLECULAR DOCKING SIMULATION; MUTAGENICITY TESTS; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN ISOFORMS; PROTEIN KINASE INHIBITORS; PURINES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84881373454     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.06.052     Document Type: Article

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