Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors |
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| Affiliation: | 1. Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia;2. Università degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy;3. Leibniz Institute for Catalysis, Albert-Einstein-Straße 29a, 18059 Rostock, Germany;4. Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, 3/7 Paula Valdena Str., Riga LV-1048, Latvia;1. Department of Biomedical Sciences for Health, University of Milan, Via Mangiagalli 31, 20133 Milan, Italy;2. Department of Biomedical, Surgical and Dental Sciences, University of Milan, 20133 Milan, Italy;3. Laboratory of Stem Cells for Tissue Engineering, IRCCS Policlinico San Donato, Piazza Malan 2, San Donato Milanese, 20097 Milan, Italy;4. Department of Internal Medicine and Therapeutics, University of Pavia, Pavia, Italy;5. IRCCS Mondino Foundation, Pavia, Italy;6. University of Vita-Salute San Raffaele, Milan, Italy;1. State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People''s Republic of China;2. State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, Nanjing, People''s Republic of China;3. Department of Pharmacology of Chinese Materia Medica, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People''s Republic of China;1. School of Chemistry, University of Manchester, Oxford Road, Manchester M13 9PL, UK;2. School of Environment and Life Sciences, University of Salford, Salford M5 4WT, UK;3. Institute of Cancer Therapeutics, University of Bradford, Richmond Road, Bradford BD7 1DP, UK;4. Manchester Pharmacy School, University of Manchester, Oxford Road, Manchester M13 9PT, UK |
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| Abstract: | Benzoxepinones (“homocoumarins”) are identified as a new class of selective inhibitors for tumor associated human carbonic anhydrases (hCA, EC 4.2.1.1) isoforms IX and XII. Similar to coumarins, they do not inhibit or poorly inhibit cytosolic human (h) isoforms hCA I and II, but act as nanomolar inhibitors of the trans-membrane, tumor associated isoforms hCA IX and XII. |
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| Keywords: | Carbonic anhydrase Benzoxepinone Selective inhibitor Tumor Catalytic Wittig reaction |
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