New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: Synthesis,spectroscopic studies,and biological activity |
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| Affiliation: | 1. Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia, Alexandria 21321, Egypt;2. Bacteriology Unit, Botany Department, Faculty of Science, Tanta University, Tanta 31527, Egypt;3. Department of Chemistry, College of Science, King Saud University, P. O. Box 2455, Riyadh 11451, Saudi Arabia;1. National Institute of Chemistry, Hajdrihova 19, 1001 Ljubljana, Slovenia;2. National Institute of Biology, Department of Genetic Toxicology and Cancer Biology, Večna pot 111, 1000 Ljubljana, Slovenia;1. Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia, Alexandria 21321, Egypt;2. Bacteriology Unit, Botany Department, Faculty of Science, Tanta University, Tanta 31527, Egypt;3. Department of Chemistry, College of Science, King Saud University, P. O. Box 2455, Riyadh 11451, Saudi Arabia;1. Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Egypt;2. Department of Oncologic Sciences, USA Mitchell Cancer Institute, 1660 Springhill Avenue, Mobile, AL 36604, USA;3. School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3NB, Wales, UK;1. Institute of Ion Physics and Applied Physics, University of Innsbruck, A-6020 Innsbruck, Austria;2. Kazan National Research Technological University, 420015 Kazan, Republic of Tatarstan, Russian Federation;3. Department of Chemistry, York University, Toronto, ON M3J 1P3, Canada |
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| Abstract: | New benzothieno[3,2-d]-1,2,3-triazines, together with precursors triazenylbenzo[b]thiophenes, were designed, synthesized and screened as anticancer agents. The structural features of these compounds prompted us to investigate their DNA binding capability through UV–vis absorption titrations, circular dichroism, and viscometry, pointing out the occurrence of groove-binding. The derivative 3-(4-methoxy-phenyl)benzothieno[3,2-d]-1,2,3-triazin-4(3H)-one showed the highest antiproliferative effect against HeLa cells and was also tested in cell cycle perturbation experiments. The obtained results assessed for the first time the anticancer activity of benzothieno[3,2-d]-1,2,3-triazine nucleus, and we related it to its DNA-binding properties. |
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| Keywords: | Benzothienotriazines Antiproliferative activity Spectroscopic studies Cell-cycle analysis VLAK |
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