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New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

Autor: Okoye-Okafor UC; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Bartholdy B; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Cartier J; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Gao EN; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Pietrak B; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Rendina AR; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Rominger C; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Quinn C; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Smallwood A; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Wiggall KJ; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Reif AJ; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Schmidt SJ; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Qi H; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Zhao H; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Joberty G; Cellzome, Heidelberg, Germany., Faelth-Savitski M; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Bantscheff M; Cellzome, Heidelberg, Germany., Drewes G; Cellzome, Heidelberg, Germany., Duraiswami C; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Brady P; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Groy A; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Narayanagari SR; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Antony-Debre I; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Mitchell K; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Wang HR; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Kao YR; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Christopeit M; Department of Stem Cell Transplantation, University Medical Center, Hamburg, Germany., Carvajal L; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Barreyro L; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Paietta E; Division of Hemato-Oncology, Department of Medicine (Oncology), Albert Einstein College of Medicine / Montefiore Medical Center, Bronx, New York, USA., Makishima H; Taussig Cancer Institute, Cleveland Clinic, Cleveland, Ohio, USA., Will B; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA., Concha N; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Adams ND; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Schwartz B; Department of Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania, USA., McCabe MT; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, Pennsylvania, USA., Maciejewski J; Taussig Cancer Institute, Cleveland Clinic, Cleveland, Ohio, USA., Verma A; Division of Hemato-Oncology, Department of Medicine (Oncology), Albert Einstein College of Medicine / Montefiore Medical Center, Bronx, New York, USA.; Department of Developmental &Molecular Biology, Albert Einstein College of Medicine, Bronx, New York, USA.; Albert Einstein Cancer Center, Albert Einstein College of Medicine, Bronx, New York, USA.; Gottesman Institute for Stem Cell and Regenerative Medicine Research, Albert Einstein College of Medicine, Bronx, New York, USA., Steidl U; Department of Cell Biology, Albert Einstein College of Medicine, Bronx, New York, USA.; Division of Hemato-Oncology, Department of Medicine (Oncology), Albert Einstein College of Medicine / Montefiore Medical Center, Bronx, New York, USA.; Albert Einstein Cancer Center, Albert Einstein College of Medicine, Bronx, New York, USA.; Gottesman Institute for Stem Cell and Regenerative Medicine Research, Albert Einstein College of Medicine, Bronx, New York, USA.

Publikováno v: Nature chemical biology [Nat Chem Biol] 2015 Nov; Vol. 11 (11), pp. 878-86. Date of Electronic Publication: 2015 Oct 05.

Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors.

Autor: Tedesco R; Department of Medicinal Chemistry, GlaxoSmithKline Pharmaceuticals, Collegeville, PA 19426, USA. Rosanna_2_Tedesco@gsk.com, Chai D, Darcy MG, Dhanak D, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Sarisky RT, Shaw AN, Valko KL, Wiggall KJ, Zimmerman MN, Duffy KJ

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Aug 01; Vol. 19 (15), pp. 4354-8. Date of Electronic Publication: 2009 May 27.