About: Synthesis, Characterization and in Vitro Antitumor Activity of Platinum(II) Oxalato Complexes Involving 7-Azaindole Derivatives as Coligands     Goto   Sponge   NotDistinct   Permalink

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Description
  • The platinum(II) oxalato complexes [Pt(ox)(naza)(2)] (1-3) were synthesized and characterized by elemental analysis (C, H, N), multinuclear NMR spectroscopy (H-1, C-13, N-15, Pt-195) 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 uM, and 18.3 uM, 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 uM), HeLa (IC50 = 31.8 uM) and A2780 (IC50 = 19.2 uM) 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.
  • The platinum(II) oxalato complexes [Pt(ox)(naza)(2)] (1-3) were synthesized and characterized by elemental analysis (C, H, N), multinuclear NMR spectroscopy (H-1, C-13, N-15, Pt-195) 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 uM, and 18.3 uM, 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 uM), HeLa (IC50 = 31.8 uM) and A2780 (IC50 = 19.2 uM) 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. (en)
Title
  • Synthesis, Characterization and in Vitro Antitumor Activity of Platinum(II) Oxalato Complexes Involving 7-Azaindole Derivatives as Coligands
  • Synthesis, Characterization and in Vitro Antitumor Activity of Platinum(II) Oxalato Complexes Involving 7-Azaindole Derivatives as Coligands (en)
skos:prefLabel
  • Synthesis, Characterization and in Vitro Antitumor Activity of Platinum(II) Oxalato Complexes Involving 7-Azaindole Derivatives as Coligands
  • Synthesis, Characterization and in Vitro Antitumor Activity of Platinum(II) Oxalato Complexes Involving 7-Azaindole Derivatives as Coligands (en)
skos:notation
  • RIV/61989592:15310/14:33152618!RIV15-MSM-15310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(ED2.1.00/03.0058), P(GAP207/11/0841), S
http://linked.open...iv/cisloPeriodika
  • 8
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 49005
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15310/14:33152618
http://linked.open...riv/jazykVysledku
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  • antitumor activity; multinuclear NMR; 7-azaindole derivatives; oxalato complexes; platinum(II) complexes (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • CH - Švýcarská konfederace
http://linked.open...ontrolniKodProRIV
  • [671DC223E56F]
http://linked.open...i/riv/nazevZdroje
  • Molecules
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 19
http://linked.open...iv/tvurceVysledku
  • Dvořák, Zdeněk
  • Trávníček, Zdeněk
  • Štarha, Pavel
  • Popa, Igor
http://linked.open...ain/vavai/riv/wos
  • 000341502600008
issn
  • 1420-3049
number of pages
http://bibframe.org/vocab/doi
  • 10.3390/molecules190810832
http://localhost/t...ganizacniJednotka
  • 15310
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