2. Academic Validation
  3. New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: synthesis, spectroscopic studies, and biological activity

New benzothieno[3,2-d]-1,2,3-triazines with antiproliferative activity: synthesis, spectroscopic studies, and biological activity

  • Bioorg Med Chem Lett. 2014 Aug 1;24(15):3291-7. doi: 10.1016/j.bmcl.2014.06.007.
Antonino Lauria 1,  Alessia Alfio 2,  Riccardo Bonsignore 2,  Carla Gentile 2,  Annamaria Martorana 2,  Giuseppe Gennaro 2,  Giampaolo Barone 2,  Alessio Terenzi 2,  Anna Maria Almerico 2
Affiliations

Affiliations

  • 1 Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo-Via Archirafi, 32-90123 Palermo, Italy. Electronic address: antonino.lauria@unipa.it.
  • 2 Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo-Via Archirafi, 32-90123 Palermo, Italy.
PMID: 24986661 DOI: 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.

Keywords

Antiproliferative activity; Benzothienotriazines; Cell-cycle analysis; Spectroscopic studies; VLAK.

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