Search results for: BENZOXATHIOLE

• Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives

  Publication

  • M. T. Konieczny
  • A. Bułakowska
  • J. Polak
  • D. Pirska
  • W. Konieczny
  • P. Gryń
  • A. Składanowski
  • M. Sabisz
  • K. Lemke
  • A. Pieczykolan... and 3 others

  - Chemical Biology & Drug Design - Year 2014

  Derivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...

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• Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin

  Publication

  • M. T. Konieczny
  • A. Buɬakowska
  • D. Pirska
  • W. Konieczny
  • A. Składanowski
  • M. Sabisz
  • M. Wojciechowski
  • K. Lemke
  • A. Pieczykolan
  • W. Strożek

  - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY - Year 2015

  Synthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...

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