Design and evaluation of biological activity of diazenecarboxamide-extended cisplatin and carboplatin analogues

Stojanović, Nikolina; Urankar, Damjana; Brozović, Anamaria; Ambriović-Ristov, Andreja; Osmak, Maja; Košmrlj, Janez (2013) Design and evaluation of biological activity of diazenecarboxamide-extended cisplatin and carboplatin analogues. Acta Chimica Slovenica, 60 (2). pp. 368-374. ISSN 1318-0207

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Abstract

Construction of a library of structurally diverse diazenecarboxamide-extended cis-[Pt(2-picolyl-1,2,3-triazole)Cl-2] 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 mu M, comparable to that of cisplatin (IC50 = 16.3 mu M).

Item Type:	Article
Uncontrolled Keywords:	cisplatin; carboplatin; diazenecarboxamide; glutathione; anti-cancer activity
Subjects:	NATURAL SCIENCES > Biology
Divisions:	Division of Molecular Biology
Projects:	Project title Project leader Project code Project type Stanični odgovor na citotoksične spojeve i razvoj otpornosti- Maja Osmak 098-0982913-2748 MZOS Povećanje transdukcije adenovirusnih vektora i otpornost stanica na citostatike- Andreja Ambriović Ristov 098-0982913-2850 MZOS
Depositing User:	Maja Osmak
Date Deposited:	16 Sep 2016 11:54
URI:	http://fulir.irb.hr/id/eprint/3042

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