A Cu(ii) complex targeting the translocator protein: in vitro and in vivo antitumor potential and mechanistic insights

Abstract

A new Cu-based anticancer metallodrug which targets the translocator protein is reported. [CuBr2(TZ6)] elicits a remarkable in vitro cytotoxicity in sensitive and multidrug resistant cell lines and induces a 98% reduction of tumor mass in a murine tumor model. Target binding was studied by experimental and computational methods

Copper Complex Nanoformulations Featuring Highly Promising Therapeutic Potential in Murine Melanoma Models

“…The widespread success of the Pt(II) complex cisplatin in the clinic for the treatment of various tumours has placed coordination chemistry of metal-based drugs in the frontline for fighting cancer [2]. In this field, copper-based complexes (mostly Cu 2+ ; Figure 1) have been investigated as new generation metallodrugs on the assumption that endogenous metals may be less toxic for normal cells with respect to cancer cells [3,4]. For example, the cytotoxic dinuclear Cu 2+ complex [Cu(phen)2] + (phen = 1,10-phenanthroline) has been reported to bind at the minor groove of DNA and to mediate single-stranded breaks through oxidation of deoxyribose [5].…”

Designing anticancer copper(II) complexes by optimizing 2-pyridine-thiosemicarbazone ligands

“…Copper, as the active centre of many enzymes, plays an important role in development and function of human organs and tissues [20][21][22]. To date, copper-based complexes have been extensively synthesised and investigated as anticancer agents because of their high antitumor activity and advantages relative to other metal anticancer complexes [23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38]. Thiosemicarbazones are formed by a condensation reaction of thiosemicarbazide and aldehydes or ketones.…”

Synthesis and Cytotoxic Activity Evaluation of New Cu(I) Complexes of Bis(pyrazol-1-yl) Acetate Ligands Functionalized with an NMDA Receptor Antagonist

“…Supplementary Materials: Supplementary materials can be found at http://www.mdpi.com/1422-0067/21/7/2616/ s1. Figure S1: Spectra of solutions containing ctDNA (0.14 mM) and increasing concentrations of ligands and related complexes 1-8 in Tris-HCl buffer, pH = 7.3; Figure S2: 13 C-NMR spectra of L H and L 2 H; Figure S3: 13 C-NMR spectra of L NMDA and L 2NMDA ; Figure S4: 1 H-NMR and 13 C-NMR spectra of 1; Figure S5: 1 H-NMR spectrum of 3; Figure S6: 1 H-NMR spectrum of 5; Figure S7: 1 H-NMR spectrum of 6; Figure S8: 1 H-NMR, 13 C-NMR, and C/H COSY spectra of 7; Figure S9: 1 H-NMR, 13 C-NMR, and C/H COSY spectra of 8.…”

“…Recent screenings on the anticancer potential of copper complexes showed promising in vitro and in vivo results [11][12][13][14][15][16][17][18][19][20], and they are currently receiving significant attention. Actually, the raised need for copper by cancer tissues and the established role of copper as a limiting factor for multiple aspects of tumor progression, including growth, angiogenesis, and metastasis, laid down the basis for the development of copper complexes as anticancer agents [12,[21][22][23].…”