Cover Image

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

Nikolina Stojanović, Damijana Urankar, Anamaria Brozović, Andreja Ambriović-Ristov, Maja Osmak, Janez Košmrlj

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).


Keywords


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

Full Text:

PDF

Refbacks

  • There are currently no refbacks.


Copyright (c) 2013 Nikolina Stojanović, Damijana Urankar, Anamaria Brozović, Andreja Ambriović-Ristov, Maja Osmak, Janez Košmrlj

Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 International License.