Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives |
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| Institution: | 1. Auckland Cancer Society Research Centre, The University of Auckland, New Zealand;2. Department of Molecular Medicine and Pathology, The University of Auckland, New Zealand;3. School of Chemical Sciences, The University of Auckland, New Zealand;1. Institute of Pharmaceutical Chemistry and MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences, University of Szeged, H-6720 Szeged, Eötvös u. 6, Hungary;2. Department of Chemistry, University of Potsdam, Karl-Liebknecht-Str. 24-25, D-14476 Potsdam, Golm, Germany;1. School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, POB 1627, 70211 Kuopio, Finland;2. Departments of Pharmacology and Toxicology and Psychiatry, University of Toronto, Campbell Family Mental Health Research Institute, M5S 1A8 Toronto, Ontario, Canada;1. School of Chemistry, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland;2. Irish Centre of High-End Computing, Grand Canal Quay, Dublin 2, Ireland;3. Department of Pharmacology, University of the Basque Country UPV/EHU, Centro de Investigación Biomédica en Red de Salud Mental, CIBERSAM, Spain;1. Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L.Mnjoyan, Ave. Azatutyan 26, Yerevan 0014, Armenia;2. Dipartimento di Chimica G. Ciamician, Alma Mater Studiorum-Università di Bologna, Via F. Selmi 2, Bologna 40126, Italy;3. Aristotle University of Thessaloniki, School of Pharmacy, Thessaloniki 54124, Greece;1. Normandie Univ, COBRA, UMR 6014 & FR 3038; Univ Rouen; INSA Rouen; CNRS, Bâtiment IRCOF, 1 rue Tesnière, 76821 Mont St Aignan Cedex, France;2. Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICiMed UPRES EA 1155, UFR des Sciences Pharmaceutiques et Biologiques, 1 rue Gaston Veil, 44035 Nantes, France;3. Protein Phosphorylation & Human Disease Group, Station Biologique, 29680 Roscoff, France;4. Manros Therapeutics, Centre de Perharidy, 29680 Roscoff, France;1. State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116023, China;2. WPI-Advanced Institute for Materials Research (WPI-AIMR), Tohoku University, Sendai 980-8577, Japan |
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| Abstract: | Seventy nine derivatives of thieno2,3-b]quinolines, tetrahydrothieno2,3-b]quinoline, dihydrocyclopentab]thieno3,2-e]pyridine, cycloheptab]thieno3,2-e]pyridine and hexahydrocyclooctab]thieno3,2-e]pyridine were either synthesized or obtained commercially and tested for their antiproliferative activity against HCT116, MDA-MB-468 and MDA-MB-231 human cancer cell lines. The most potent eight compounds were active against all cell lines with IC50 values in the 80–250 nM range. In general hexahydrocyclooctab]thieno3,2-e]pyridines were most active with increasing activity observed as larger cycloalkyl rings were fused to the pyridine ring. |
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| Keywords: | Antiproliferative |
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