Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.

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Title: Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.
Authors: Rohde JM; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA. Electronic address: jason.rohde@nih.gov., Brimacombe KR; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Liu L; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Pacold ME; Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA; Howard Hughes Medical Institute, Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Koch Institute for Integrative Cancer Research, 77 Massachusetts Avenue, Cambridge, MA 02139, USA; Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, MA 02142, USA; Dana-Farber Cancer Institute, Longwood Center, 350 Longwood Avenue, Boston, MA 02215, USA; Department of Radiation Oncology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA., Yasgar A; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Cheff DM; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Lee TD; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Rai G; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Baljinnyam B; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Li Z; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Simeonov A; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Hall MD; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Shen M; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA., Sabatini DM; Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA; Howard Hughes Medical Institute, Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Koch Institute for Integrative Cancer Research, 77 Massachusetts Avenue, Cambridge, MA 02139, USA; Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, MA 02142, USA., Boxer MB; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.
Source: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2018 May 01; Vol. 26 (8), pp. 1727-1739. Date of Electronic Publication: 2018 Feb 27.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Journal Info: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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PubType: Academic Journal
PubTypeId: academicJournal
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  Data: Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors.
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  Data: <searchLink fieldCode="AU" term="%22Rohde+JM%22">Rohde JM</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA. Electronic address: jason.rohde@nih.gov.<br /><searchLink fieldCode="AU" term="%22Brimacombe+KR%22">Brimacombe KR</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Liu+L%22">Liu L</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Pacold+ME%22">Pacold ME</searchLink>; Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA; Howard Hughes Medical Institute, Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Koch Institute for Integrative Cancer Research, 77 Massachusetts Avenue, Cambridge, MA 02139, USA; Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, MA 02142, USA; Dana-Farber Cancer Institute, Longwood Center, 350 Longwood Avenue, Boston, MA 02215, USA; Department of Radiation Oncology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA.<br /><searchLink fieldCode="AU" term="%22Yasgar+A%22">Yasgar A</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Cheff+DM%22">Cheff DM</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Lee+TD%22">Lee TD</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Rai+G%22">Rai G</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Baljinnyam+B%22">Baljinnyam B</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Li+Z%22">Li Z</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Simeonov+A%22">Simeonov A</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Hall+MD%22">Hall MD</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Shen+M%22">Shen M</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.<br /><searchLink fieldCode="AU" term="%22Sabatini+DM%22">Sabatini DM</searchLink>; Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA; Howard Hughes Medical Institute, Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA; Koch Institute for Integrative Cancer Research, 77 Massachusetts Avenue, Cambridge, MA 02139, USA; Broad Institute of Harvard and Massachusetts Institute of Technology, 7 Cambridge Center, Cambridge, MA 02142, USA.<br /><searchLink fieldCode="AU" term="%22Boxer+MB%22">Boxer MB</searchLink>; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA.
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  Data: <searchLink fieldCode="JN" term="%229413298%22">Bioorganic & medicinal chemistry</searchLink> [Bioorg Med Chem] 2018 May 01; Vol. 26 (8), pp. 1727-1739. <i>Date of Electronic Publication: </i>2018 Feb 27.
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        Value: 10.1016/j.bmc.2018.02.016
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      – Code: eng
        Text: English
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