Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
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| Title: | Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists. |
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| Authors: | Orsi DL; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Ferrara SJ; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Siegel S; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Friberg A; Nuvisan ICB GmbH, 13353 Berlin, Germany., Bouché L; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Pook E; Research and Development, Pharmaceuticals, Bayer AG, 42113 Wuppertal, Germany., Lienau P; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Bluck JP; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Lemke CT; Center for the Development of Therapeutics, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Akcay G; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Stellfeld T; Nuvisan ICB GmbH, 13353 Berlin, Germany., Meyer H; Nuvisan ICB GmbH, 13353 Berlin, Germany., Pütter V; Nuvisan ICB GmbH, 13353 Berlin, Germany., Holton SJ; Nuvisan ICB GmbH, 13353 Berlin, Germany., Korr D; Nuvisan ICB GmbH, 13353 Berlin, Germany., Jerchel-Furau I; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Pantelidou C; Bayer US LLC, Research and Development Precision Molecular Oncology, Cambridge, MA 02142, USA., Strathdee CA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA., Meyerson M; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Center for Cancer Genomics, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Genetics and Medicine, Harvard Medical School, Boston, MA 02115, USA., Eis K; Research and Development, Pharmaceuticals, Bayer AG, 13353 Berlin, Germany., Goldstein JT; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA. Electronic address: jgold@broadinstitute.org. |
| Source: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2023 Jan 15; Vol. 78, pp. 117130. Date of Electronic Publication: 2022 Dec 13. |
| 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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