Synthesis and Topoisomerase I inhibitory properties of klavuzon derivatives |
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| Affiliation: | 1. İzmir Institute of Technology, Faculty of Science, Department of Chemistry, Urla 35430, İzmir, Turkey;2. İzmir Institute of Technology, Faculty of Science, Department of Molecular Biology and Genetics, Urla 35430, İzmir, Turkey;3. Department of Bioengineering, Cancer Biology Laboratory, Faculty of Engineering, Ege University, Bornova, İzmir, Turkey;1. Institute of Organic Chemistry, National Academy of Sciences of Ukraine, 5 Murmans’ka str., Kyiv 02660, Ukraine;2. Department of Organic Chemistry, National Technical University of Ukraine ‘Kyiv Polytechnic Institute’, 37, Prospect Peremogy, Kyiv 03056, Ukraine;1. Chemistry and Chemical Engineering School, Henan University of Technology, Zhengzhou, Henan 450001, PR China;2. School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, PR China;1. Faculty of Chemistry, University of Wrocław, F. Joliot-Curie 14, 50-383 Wrocław, Poland;2. Department of Chemistry, Taras Shevchenko National University of Kyiv, Volodymyrska 60, 01601 Kiev, Ukraine;3. Department of Chemistry, University of Jyväskylä, Seminaarinkatu 15 (C building), FI-40100 Jyväskylä, Finland |
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| Abstract: | Klavuzon is a naphthalen-1-yl substituted α,β-unsaturated δ-lactone derivative, and is one of the anti-proliferative members of this class of compounds. Asymmetric and racemic syntheses of novel α,β-unsaturated δ-lactone derivatives are important to investigate their potential for the treatment of cancer. In this study, asymmetric and racemic syntheses of heteroatom-substituted klavuzon derivatives are reported. The syntheses were completed by a well-known three-step procedure. Anti-proliferative activity of seven novel racemic klavuzon derivatives were reported against MCF-7, PC3, HCT116 p53+/+ and HCT116 p53−/− cancer cell lines. Topoisomerase I inhibitory properties of 5,6-dihydro-2H-pyran-2-one derivatives were also studied. |
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| Keywords: | α,β-Unsaturated δ-lactone Klavuzon Anti-proliferative activity |
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