title: Synthesis, characterization and in vitro antitumor activity of platinum(II) oxalato complexes involving 7-azaindole derivatives as coligands.
abstract: The platinum(II) oxalato complexes [Pt(ox)(naza)2] (1-3) were synthesized and characterized by elemental analysis (C, H, N), multinuclear NMR spectroscopy ((1)H, (13)C, (15)N, (195)Pt) and electrospray ionization mass spectrometry (ESI-MS); naza = 4-chloro-7-azaindole (4Claza; 1), 3-bromo-7-azaindole (3Braza; 2) or 4-bromo-7-azaindole (4Braza; 3). The prepared substances were screened for their in vitro antitumor activity on the osteosarcoma (HOS) and breast adenocarcinoma (MCF7) human cancer cell lines, where 2 showed moderate antitumor effect (IC50 = 27.5 μM, and 18.3 μM, respectively). The complex 2 was further tested on a panel of six others human cancer cell lines, including the malignant melanoma (G361), cervix carcinoma (HeLa), ovarian carcinoma (A2780), cisplatin-resistant ovarian carcinoma (A2780R), lung carcinoma (A549) and prostate adenocarcinoma (LNCaP). This substance was found to be moderate antitumor effective against G361 (IC50 = 17.3 μM), HeLa (IC50 = 31.8 μM) and A2780 (IC50 = 19.2 μM) cell lines. The complex 2 was also studied by NMR for its solution stability and by ESI-MS experiments for its ability to interact with biomolecules, such as cysteine, glutathione or guanosine 5'-monophosphate.
authors: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University, 17. listopadu 12, CZ 77146 Olomouc, Czech Republic.
authors: Pavel
authors: P
authors: Štarha
authors: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University, 17. listopadu 12, CZ 77146 Olomouc, Czech Republic. zdenek.travnicek@upol.cz.
authors: Zdeněk
authors: Z
authors: Trávníček
authors: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University, 17. listopadu 12, CZ 77146 Olomouc, Czech Republic. igor.popa@upol.cz.
authors: Igor
authors: I
authors: Popa
authors: Regional Centre of Advanced Technologies and Materials, Department of Cell Biology and Genetics, Faculty of Science, Palacký University, Šlechtitelů 11, CZ 78371 Olomouc, Czech Republic. zdenek.dvorak@upol.cz.
authors: Zdeněk
authors: Z
authors: Dvořák
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010070:Oxalates / Q000737:chemistry*
chemical_list: C023422:7-azaindole dimer; D000970:Antineoplastic Agents; D007211:Indoles; D009944:Organoplatinum Compounds; D010070:Oxalates