Please use this identifier to cite or link to this item: http://hdl.handle.net/11452/32399
Title: Structures and anticancer activity of chlorido platinum(II) saccharinate complexes with mono- and dialkylphenylphosphines
Authors: Cevatemre, Buse
Aygun, Muhittin
Ulukaya, Engin
Bursa Uludağ Üniversitesi/Fen-Edebiyat Fakültesi/Kimya, Anorganik Kimya Bölümü.
0000-0002-2849-3332
0000-0002-2717-2430
İçsel, Ceyda
Yılmaz, Veysel Turan
L-7238-2018
AAI-3342-2021
55551960400
56441123900
Keywords: Pt(II) complex
Saccharinate
Phosphine
DNA binding
Cytotoxicity
Anticancer mechanism
Ascites-carcinoma eac
Antiproliferative activity
Phosphorus Ligands
Antitumor-activity
Phosphine-Ligands
In-Vitro
Palladium(II)
DNA
Cislatin
Terpyridine
Biochemistry & molecular biology
Chemistry
Issue Date: Jun-2019
Publisher: Elsevier
Citation: İçsel, C. vd. (2019). ''Structures and anticancer activity of chlorido platinum(II) saccharinate complexes with mono- and dialkylphenylphosphines''. Journal of Inorganic Biochemistry, 195, 39-50.
Abstract: Cis-[PtCl(sac)(PPh2Me)(2)] (1), cis-[PtCl(sac)(PPhMe2)(2)] (2), trans-[PtCl(sac)(PPh2Et)(2)] (3) and trans- [PtCl(sac) (PPhEt2)(2)] (4) complexes (sac = saccharinate) were synthesized and characterized by elemental analysis and spectroscopic methods. The structures of 2-4 were determined by X-ray single-crystal diffraction. The interaction of the complexes with DNA was studied various biochemical, biophysical and molecular docking methods. Only the cis-configured complexes (1 and 2) showed nuclease activity and their binding affinity towards DNA was considerably higher than those of their trans-congeners (3 and 4). The chlorido ligand in the cis-configured complexes underwent aquation, making them more reactive towards DNA. Furthermore, 1 and 2 exhibited anticancer potency on breast (MCF-7) and colon (HCT116) cancer cells similar to cisplatin, whereas 3 and 4 were biologicallly inactive. Mechanistic studies on MCF-7 cells showed that higher nuclear uptake, cell cycle arrest at the S phase, dramatically increased DNA double-strand breaks, apoptosis induction, elevated levels of reactive oxygen species (ROS) and high mitochondrial membrane depolarization greatly contribute to the anticancer potency of 1 and 2.
URI: https://doi.org/10.1016/j.jinorgbio.2019.03.008
https://www.sciencedirect.com/science/article/pii/S0162013419300650
http://hdl.handle.net/11452/32399
ISSN: 0162-0134
1873-3344
Appears in Collections:Scopus
Web of Science

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