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      Benzothiazole derivatives as human DNA topoisomerase IIα inhibitors

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      Author
      Kaplan-Ozen, C.
      Tekiner-Gulbas, B.
      Foto, E.
      Yildiz I.
      Diril, N.
      Aki, E.
      Yalcin I.
      Date
      2013
      Journal Title
      Medicinal Chemistry Research
      ISSN
      10542523
      Volume
      22
      Issue
      12
      Pages
      5798 - 5808
      Language
      English
      Type
      Article
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      Please cite this item using this persistent URL
      http://hdl.handle.net/11693/20709
      Abstract
      Benzothiazole derivatives resembling the structure of DNA purine bases were tested to determine their topoisomerase inhibition activities. Based on DNA topoisomerase I and II relaxation assay results, all 12 derivatives acted as human topoisomerase IIα inhibitors, whereas only two compounds inhibited Calf thymus topoisomerase I. 3-amino-2-(2-bromobenzyl)-1,3-benzothiazol-3-ium 4-methylbenzensulfonate (BM3) was observed to be the most effective human topoisomerase IIα inhibitor with the lowest IC50 value of 39 nM. The mechanistic studies suggested that BM3 was neither a DNA intercalator nor a topoisomerase poison, it was only a DNA minor groove-binding agent. BM3 initially bound to the DNA topoisomerase IIα enzyme, then to DNA. As a result, the tested benzothiazole derivatives were obtained as strong topoisomerase IIα inhibitors. The benzothiazole tosylated salt form BM3 was found as the most effective topoisomerase IIα inhibitor. BM3's mechanisms of action might be its direct interaction with the enzyme. BM3's minor groove-binding property might also contribute to this action. Hence, BM3 could be a good candidate as a new anticancer agent. © 2013 Springer Science+Business Media New York.
      Published as
      http://dx.doi.org/10.1007/s00044-013-0577-5
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