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The synthesis of trifluoromethylated N-nitroaryl-2-amino-1,3-dichloropropane derivatives and their evaluation as potential anti-cancer agents
Institution:1. School of Marine Science and Technology, Harbin Institute of Technology, Weihai, 2# Wenhua West Road, Weihai, 264209, PR China;2. State Key Laboratory of Urban Water Resource and Environment, Harbin Institute of Technology, 73# Huanghe Road, Harbin, 150090, PR China;3. Guangzhou Key Laboratory of Environmental Exposure and Health, School of Environment, Jinan University, Guangzhou, 510632, PR China;4. Weihai Blood Center, 28# Qingdao North Road, Weihai, 264200, PR China;1. Taiwan International Graduate Program, Taiwan, ROC;2. Institute of Chemistry, Academia Sinica, 128 Section 2 Academia Road, Nankang, Taipei 11529, Taiwan, ROC;3. Department of Chemistry, National Tsing Hua University, 101 Section 2 Kuang-Fu Road, Hsinchu 30031, Taiwan, ROC;4. Department of Photonics, National Sun Yat-Sen University, Kaohsiung 804, Taiwan, ROC;1. Medicinal Chemistry, Biogen, 225 Binney Street, Cambridge, MA 02142, USA;2. Biophysics, Biogen, 225 Binney Street, Cambridge, MA 02142, USA;3. Drug Metabolism & Pharmacokinetics, Biogen, 225 Binney Street, Cambridge, MA 02142, USA;4. Research & Early Development, Biogen, 225 Binney Street, Cambridge, MA 02142, USA;1. Université de Rennes 1, Institut des Sciences Chimiques de Rennes, CNRS UMR 6226, Avenue du Général Leclerc, 35042 Rennes Cedex, France;2. UMR 892 INSERM/6299 CNRS/Université de Nantes, Team 8 “Cell survival and tumor escape in breast cancer”, Institut de Recherche Thérapeutique de l’Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France;3. Institut de Cancérologie de l’Ouest, Centre de Lutte contre le Cancer René Gauducheau, Boulevard Jacques Monod, 44805 Saint Herblain-Nantes Cedex, France;4. Plateforme IMPACT®, Biogenouest Institut de Recherche Thérapeutique de l’Université de Nantes, 8 quai Moncousu, BP 70721, 44007 Nantes Cedex 1, France;5. Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint Grégoire, France
Abstract:Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature associated with the compounds’ cytotoxicities.
Keywords:Nitroaromatic drugs  Anti-cancer agents  Trifluoromethylated drugs  Nitrogen mustards
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