Design and Evaluation of Biological Activity of Diazenecarboxamide-extended Cisplatin...

Authors

  • Nikolina Stojanović Division of Molecular Biology, Ruder Bošković Institute, Zagreb, Croatia;
  • Damijana Urankar Faculty of Chemistry and Chemical Technology, University of Ljubljana, Slovenia
  • Anamaria Brozović Division of Molecular Biology, Ruder Bošković Institute, Zagreb, Croatia;
  • Andreja Ambriović-Ristov Division of Molecular Biology, Ruder Bošković Institute, Zagreb, Croatia;
  • Maja Osmak Division of Molecular Biology, Ruder Bošković Institute, Zagreb, Croatia;
  • Janez Košmrlj Faculty of Chemistry and Chemical Technology, University of Ljubljana, Slovenia

Keywords:

Cisplatin, carboplatin, diazenecarboxamide, glutathione, anti-cancer activity

Abstract

Construction of a library of structurally diverse diazenecarboxamide-extended cis-[Pt(2-picolyl-1,2,3-triazole)Cl2,] and cis-[Pt(propan-1,3-diamine)CBDCA] (CBDCA = 1,1 -cyclobutanedicarboxylate) complexes 1-4 is described. These compounds retain oxidative properties of parent diazenecarboxamides against glutathione as demonstrated by NMR spectroscopy and high resolution mass spectrometry experiments. Cytotoxic activity of 1-4 was investigated against human cervical carcinoma HeLa cells. Four library members were found to possess moderate cytotoxic activity. Some model compounds were also examined, returning [PtCl2L2] (L = 1-(2-picolyl)-4-phenyl-1H-1,2,3-triazole) as the most potent under this investigation with IC50 of 19.05 microM, comparable to that of cisplatin (IC50 = 16.3 microM).

Downloads

Published

28.10.2013

Issue

Vol. 60 No. 2 (2013)

Section

Biochemistry and molecular biology

License

Except where otherwise noted, articles in this journal are published under the Creative Commons Attribution 4.0 International License