-
Something wrong with this record ?
Platinum(II) carboxylato complexes containing 7-azaindoles as N-donor carrier ligands showed cytotoxicity against cancer cell lines
P. Štarha, Z. Trávníček, L. Pazderová, Z. Dvořák,
Language English Country United States
Document type Journal Article
- MeSH
- Cell Line MeSH
- Drug Resistance, Neoplasm drug effects MeSH
- Cisplatin chemistry MeSH
- Epithelial Cells drug effects pathology MeSH
- Fibroblasts cytology drug effects MeSH
- Glutathione chemistry MeSH
- Indoles chemistry MeSH
- Inhibitory Concentration 50 MeSH
- Coordination Complexes chemical synthesis pharmacology MeSH
- G1 Phase Cell Cycle Checkpoints drug effects MeSH
- Guanosine Monophosphate chemistry MeSH
- Carboxylic Acids chemistry MeSH
- Humans MeSH
- Cell Line, Tumor MeSH
- Organoplatinum Compounds chemical synthesis pharmacology MeSH
- Antineoplastic Agents chemical synthesis pharmacology MeSH
- Cell Survival drug effects MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
The platinum(II) malonato (Mal) and decanoato (Dec) complexes of the general formulas [Pt(Mal)(naza)2] (1-3) and cis-[Pt(Dec)2(naza)2] (4-7) were prepared, characterized and tested for their in vitro cytotoxicity against cisplatin-sensitive (A2780) and cisplatin-resistant (A2780R) human ovarian carcinoma cell lines and non-cancerous human lung fibroblasts (MRC-5); naza=halogeno-derivatives of 7-azaindole. Complexes 1-7 effectively overcome the acquired resistance of ovarian carcinoma cells to cisplatin. Complexes 2 (IC50=26.6±8.9μM against A2780 and 28.9±6.7μM against A2780R), 4 (IC50=14.5±0.6μM against A2780 and 14.5±3.8μM against A2780R) and 5 (IC50=13.0±1.1μM against A2780 and 13.6±4.9μM against A2780R) indicated decreased toxicity against healthy MRC-5 cells (IC50>50.0μM for 2 and >25.0μM for 4 and 5). The representative complexes 2 and 4 showed mutually different effect on the A2780 cell cycle at IC50 concentrations after 24h exposure. Concretely, the complex 2 caused cell cycle arrest at G0/G1 phase, while 4 induced cell death by apoptosis with high population of cells in sub-G1 cell cycle phase. The hydrolysis and interactions of the selected complexes with biomolecules (glutathione (GSH) and guanosine monophosphate (GMP)) were also studied by means of (1)H NMR and ESI+ mass spectra.
References provided by Crossref.org
- 000
- 00000naa a2200000 a 4500
- 001
- bmc17031628
- 003
- CZ-PrNML
- 005
- 20171030132831.0
- 007
- ta
- 008
- 171025s2016 xxu f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.1016/j.jinorgbio.2016.06.018 $2 doi
- 035 __
- $a (PubMed)27350081
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a xxu
- 100 1_
- $a Štarha, Pavel $u Regional Centre of Advanced Technologies, Division of Biologically Active Complexes and Molecular Magnets, Faculty of Science, Palacký University, 17. listopadu 12, CZ771 46 Olomouc, Czech Republic.
- 245 10
- $a Platinum(II) carboxylato complexes containing 7-azaindoles as N-donor carrier ligands showed cytotoxicity against cancer cell lines / $c P. Štarha, Z. Trávníček, L. Pazderová, Z. Dvořák,
- 520 9_
- $a The platinum(II) malonato (Mal) and decanoato (Dec) complexes of the general formulas [Pt(Mal)(naza)2] (1-3) and cis-[Pt(Dec)2(naza)2] (4-7) were prepared, characterized and tested for their in vitro cytotoxicity against cisplatin-sensitive (A2780) and cisplatin-resistant (A2780R) human ovarian carcinoma cell lines and non-cancerous human lung fibroblasts (MRC-5); naza=halogeno-derivatives of 7-azaindole. Complexes 1-7 effectively overcome the acquired resistance of ovarian carcinoma cells to cisplatin. Complexes 2 (IC50=26.6±8.9μM against A2780 and 28.9±6.7μM against A2780R), 4 (IC50=14.5±0.6μM against A2780 and 14.5±3.8μM against A2780R) and 5 (IC50=13.0±1.1μM against A2780 and 13.6±4.9μM against A2780R) indicated decreased toxicity against healthy MRC-5 cells (IC50>50.0μM for 2 and >25.0μM for 4 and 5). The representative complexes 2 and 4 showed mutually different effect on the A2780 cell cycle at IC50 concentrations after 24h exposure. Concretely, the complex 2 caused cell cycle arrest at G0/G1 phase, while 4 induced cell death by apoptosis with high population of cells in sub-G1 cell cycle phase. The hydrolysis and interactions of the selected complexes with biomolecules (glutathione (GSH) and guanosine monophosphate (GMP)) were also studied by means of (1)H NMR and ESI+ mass spectra.
- 650 _2
- $a protinádorové látky $x chemická syntéza $x farmakologie $7 D000970
- 650 _2
- $a kyseliny karboxylové $x chemie $7 D002264
- 650 _2
- $a buněčné linie $7 D002460
- 650 _2
- $a nádorové buněčné linie $7 D045744
- 650 _2
- $a viabilita buněk $x účinky léků $7 D002470
- 650 _2
- $a cisplatina $x chemie $7 D002945
- 650 _2
- $a komplexní sloučeniny $x chemická syntéza $x farmakologie $7 D056831
- 650 _2
- $a chemorezistence $x účinky léků $7 D019008
- 650 _2
- $a epitelové buňky $x účinky léků $x patologie $7 D004847
- 650 _2
- $a fibroblasty $x cytologie $x účinky léků $7 D005347
- 650 _2
- $a kontrolní body fáze G1 buněčného cyklu $x účinky léků $7 D059585
- 650 _2
- $a glutathion $x chemie $7 D005978
- 650 _2
- $a kyselina 5'-guanylová $x chemie $7 D006157
- 650 _2
- $a lidé $7 D006801
- 650 _2
- $a indoly $x chemie $7 D007211
- 650 _2
- $a inhibiční koncentrace 50 $7 D020128
- 650 _2
- $a organoplatinové sloučeniny $x chemická syntéza $x farmakologie $7 D009944
- 650 _2
- $a vztahy mezi strukturou a aktivitou $7 D013329
- 655 _2
- $a časopisecké články $7 D016428
- 700 1_
- $a Trávníček, Zdeněk $u Regional Centre of Advanced Technologies, Division of Biologically Active Complexes and Molecular Magnets, Faculty of Science, Palacký University, 17. listopadu 12, CZ771 46 Olomouc, Czech Republic. Electronic address: zdenek.travnicek@upol.cz.
- 700 1_
- $a Pazderová, Lucia $u Regional Centre of Advanced Technologies, Division of Biologically Active Complexes and Molecular Magnets, Faculty of Science, Palacký University, 17. listopadu 12, CZ771 46 Olomouc, Czech Republic.
- 700 1_
- $a Dvořák, Zdeněk $u Regional Centre of Advanced Technologies, Division of Biologically Active Complexes and Molecular Magnets, Faculty of Science, Palacký University, 17. listopadu 12, CZ771 46 Olomouc, Czech Republic.
- 773 0_
- $w MED00006646 $t Journal of inorganic biochemistry $x 1873-3344 $g Roč. 162, č. - (2016), s. 109-116
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/27350081 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y a $z 0
- 990 __
- $a 20171025 $b ABA008
- 991 __
- $a 20171030132921 $b ABA008
- 999 __
- $a ok $b bmc $g 1255221 $s 992655
- BAS __
- $a 3
- BAS __
- $a PreBMC
- BMC __
- $a 2016 $b 162 $c - $d 109-116 $e 20160616 $i 1873-3344 $m Journal of inorganic biochemistry $n J Inorg Biochem $x MED00006646
- LZP __
- $a Pubmed-20171025
