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EnglishNew 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.
Lauria, A., Alfio, A., Bonsignore, R., Gentile, C., Martorana, A., Gennaro, G., et al. (2014). New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: Synthesis, spectroscopic studies, and biological activity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 24(24 (15)), 3291-3297 [10.1016/j.bmcl.2014.06.007].
| Data di pubblicazione: | 2014 | |
| Titolo: | New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: Synthesis, spectroscopic studies, and biological activity | |
| Autori: | ||
| Citazione: | Lauria, A., Alfio, A., Bonsignore, R., Gentile, C., Martorana, A., Gennaro, G., et al. (2014). New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: Synthesis, spectroscopic studies, and biological activity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 24(24 (15)), 3291-3297 [10.1016/j.bmcl.2014.06.007]. | |
| Rivista: | ||
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmcl.2014.06.007 | |
| 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. | |
| Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica Settore CHIM/03 - Chimica Generale E Inorganica Settore BIO/10 - Biochimica | |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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http://hdl.handle.net/10447/97019
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