New 2,6-bis-[uracil-imino] ethylpyridine complexes containing the CdN6 core: Synthesis, crystal structures, luminescent properties and antiproliferative activity against C6 glioma cells

Illán‐Cabeza, Nuria A.; Jiménez‐Pulido, Sonia B.; Martínez-Martos, José Manuel; Ramírez-Expósito, María Jesús; Moreno‐Carretero, Miguel N.

doi:10.1016/j.jinorgbio.2009.06.007

Cited by 6 publications

(1 citation statement)

References 72 publications

(73 reference statements)

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“…It seems that ligand type used for preparation of Cd complexes may cause their very favorable anti-tumor effects [17]. Ligands used for preparation of Cd complexes can be classified as: thiosemicarbazones [16,[18][19][20][21][22][23][24], selenosemicarbazones [25][26][27], hydrazones [16,[27][28][29][30][31][32][33][34][35][36], hydrazides [38,39], diimines [40], amides [41,42], aminoacids [43,44], heterocycles [44][45][46][47][48][49][50][51][52][53][54][55][56], macrocycles [58][59][60], drugs [61][62][63]…”

Section: Introductionmentioning

confidence: 99%

A novel binuclear hydrazone-based Cd(II) complex is a strong pro-apoptotic inducer with significant activity against 2D and 3D pancreatic cancer stem cells

Bjelogrlić

Todorović

Cvijetić

et al. 2019

Journal of Inorganic Biochemistry

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A novel binuclear Cd complex (1) with hydrazone-based ligand was prepared and characterized by spectroscopy and single crystal X-ray diffraction techniques. Complex 1 reveals a strong pro-apoptotic activity in both human, mammary adenocarcinoma cells (MCF-7) and pancreatic AsPC-1 cancer stem cells (CSCs). While apoptosis undergoes mostly caspase-independent, 1 stimulates the activation of intrinsic pathway with noteworthy down regulation of caspase-8 activity in respect to non-treated controls. Distribution of cells over mitotic division indicates that 1 caused DNA damage in both cell lines, which is confirmed in DNA interaction studies. Compared to 1, cisplatin (CDDP) does not achieve cell death in 2D cultured AsPC-1 cells, while induces different pattern of cell cycle changes and caspase activation in 2D cultured MCF-7 cells, implying that these two compounds do not share similar mechanism of action. Additionally, 1 acts as a powerful inducer of mitochondrial superoxide production with dissipated trans-membrane potential in the majority of the treated cells already after 6 h of incubation. On 3D tumors, 1 displays a superior activity against CSC model, and at 100 μM induces disintegration of spheroids within 2 days of incubation. Fluorescence spectroscopy, along with molecular docking show that compound 1 binds to the minor groove of DNA. Compound 1 binds to the human serum albumin (HSA) showing that the HSA can effectively transport and store 1 in the human body. Thus, our current study strongly supports further investigations on antitumor activity of 1 as a drug candidate for the treatment of highly resistant pancreatic cancer.

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