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Open AccessArticle

Simple Trans-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin

1
Department of Bioinorganic Chemistry, Medical University of Lodz, 1 Muszynskiego St., 90-151 Łódź, Poland
2
Department of Applied Pharmacy, Medical University of Warsaw, 1 Banacha St., 02–097 Warsaw, Poland
3
Theoretical and Structural Chemistry Group, Department of Physical Chemistry, Faculty of Chemistry, University of Łódź, Pomorska 163/165, 90-236 Łódź, Poland
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(6), 2116; https://doi.org/10.3390/ijms21062116
Received: 17 February 2020 / Revised: 11 March 2020 / Accepted: 17 March 2020 / Published: 19 March 2020
(This article belongs to the Section Molecular Plant Sciences)
Following previous studies devoted to trans–Pt(3-af)2Cl2, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures are presented in the Cambridge Structural Database (CSD). Molecular Hirshfeld surface analysis and computational methods were used to examine a possible relationship between the structure and anticancer activity of trans–Pt(3-af)2Cl2. The purpose of the article was also to investigate the effect of hyperthermia on the anticancer activity of cisplatin, cytostatics used in the treatment of patients with ovarian cancer and a new analogue of cisplatin-trans–Pt(3-af)2Cl2. The study was conducted on two cell lines of ovarian cancer sensitive to Caov-3 cytostatics and the OVCAR-3 resistant cisplatin line. The study used the MTT (3-(4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide) cell viability assay, LDH (lactate dehydrogenase), and the quantitative evaluation method for measuring gene expression, i.e., qPCR with TagMan probes. Reduced survivability of OVCAR-3 and Caov-3 cells exposed to cytostatics at elevated temperatures (37 °C, 40 °C, 43 °C) was observed. Hyperthermia may increase the sensitivity of cells to platinum-based antineoplastic drugs and paclitaxel, which may be associated with the reduction of gene expression related to apoptotic processes. View Full-Text
Keywords: anticancer drugs; coordination compounds; gene expression; platinum; structure–activity relationships anticancer drugs; coordination compounds; gene expression; platinum; structure–activity relationships
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Fabijańska, M.; Orzechowska, M.; Rybarczyk-Pirek, A.J.; Dominikowska, J.; Bieńkowska, A.; Małecki, M.; Ochocki, J. Simple Trans-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin. Int. J. Mol. Sci. 2020, 21, 2116.

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