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- Title
Design and Evaluation of Biological Activity of Diazenecarboxamide-extended Cisplatin and Carboplatin Analogues.
- Authors
Stojanović, Nikolina; Urankar, Damijana; Brozović, Anamaria; Ambriović-Ristov, Andreja; Osmak, Maja; Košmrlj, Janez
- 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 μM, comparable to that of cisplatin (IC50 = 16.3 μM).
- Subjects
BIOLOGICAL systems; ANTINEOPLASTIC agents; CISPLATIN; CARBOXAMIDES; DIAZENES; OXIDATIVE stress
- Publication
Acta Chimica Slovenica, 2013, Vol 60, Issue 2, p368
- ISSN
1318-0207
- Publication type
Article