New bis-pyrazolate zinc(ii) complexes as potential anticancer drugs: from structure to anticancer activity
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2025
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| author | Hasić, Rušid Kolenović Serezlić, Majda Cakovic, Angelina Bogojeski, Jovana Nikodijević,, Danijela Ćurčić Milutinović, Milena Stanojević, Aleksandra Čavić, Milena Egorov, Andrei V. Komolkin, Andrei Kornyakov, Ilya V. Scheurer, Andreas Puchta, Ralph Soldatovic, Tanja V. |
| author_facet | Hasić, Rušid Kolenović Serezlić, Majda Cakovic, Angelina Bogojeski, Jovana Nikodijević,, Danijela Ćurčić Milutinović, Milena Stanojević, Aleksandra Čavić, Milena Egorov, Andrei V. Komolkin, Andrei Kornyakov, Ilya V. Scheurer, Andreas Puchta, Ralph Soldatovic, Tanja V. |
| contents | <h3>Abstract</h3> <div> <div> <p>Three novel Zn(II) complexes <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>, <strong>[ZnCl<sub>2</sub>(Me<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> and <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> (where H<sub>2</sub>L<sup><em>t</em>Bu</sup> is 2,6-bis(5-<em>tert</em>-butyl-1<em>H</em>-pyrazol-3-yl)pyridine, Me<sub>2</sub>L<sup><em>t</em>Bu</sup> is 2,6-bis(5-<em>tert</em>-butyl-1-methyl-1<em>H</em>-pyrazol-3-yl)pyridine and H<sub>2</sub>L<sup>CatBiPyrPh</sup> is 1,2-bis((5-phenyl-1<em>H</em>-pyrazol-3-yl)methoxy)benzene) were synthesized and characterized using various spectroscopic techniques, including UV-vis, IR, <sup>1</sup>D (<sup>1</sup>H and <sup>13</sup>C) and 2D (<sup>1</sup>H–<sup>1</sup>H COSY) NMR. The structures of complexes <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> and <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> were elucidated through X-ray crystallography. The interactions of the complexes with CT-DNA and human serum albumin (HSA) were investigated using UV-vis spectroscopy and fluorescence emission titration. All examined complexes exhibited quenching constant, <em>K</em><sub>sv</sub>, values in the order of 10<sup>4</sup> with CT-DNA. Constant values followed the trend <strong>[ZnCl<sub>2</sub>(Me<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> < <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> < <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>. The results indicated a moderate interaction between the complexes and HSA. In terms of cytotoxic activity, the zinc(II) complexes significantly decreased the viability of colon (HCT-116) and pancreatic (MIA PaCa-2) cancer cell lines, where the effect on pancreatic cells after 72 h is especially emphasized. The most pronounced occurrence of apoptosis, as the dominant type of complex-induced cell death, was associated with complex <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>, while necrosis was observed at lower percentages in all investigated treatments. All complexes demonstrated downregulation of the tumor suppressor gene <em>TP53</em> (<em>homo sapiens</em> tumor protein p53). Treatment with <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> resulted in downregulation of <em>TP53</em>, <em>CASP3</em> (<em>Caspase 3</em>) and <em>IGF1R</em> (insulin-like growth factor 1), potentially impairing the effective apoptotic process and reducing cell proliferation.</p> </div> </div> |
| format | Recurso digital |
| id | zenodo_https___doi_org_10_1039_D5NJ00043B |
| institution | Zenodo |
| language | eng |
| publishDate | 2025 |
| publisher | Zenodo |
| record_format | zenodo |
| spellingShingle | New bis-pyrazolate zinc(ii) complexes as potential anticancer drugs: from structure to anticancer activity Hasić, Rušid Kolenović Serezlić, Majda Cakovic, Angelina Bogojeski, Jovana Nikodijević,, Danijela Ćurčić Milutinović, Milena Stanojević, Aleksandra Čavić, Milena Egorov, Andrei V. Komolkin, Andrei Kornyakov, Ilya V. Scheurer, Andreas Puchta, Ralph Soldatovic, Tanja V. anticancer activity anticancer drugs spectroscopic techniques <h3>Abstract</h3> <div> <div> <p>Three novel Zn(II) complexes <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>, <strong>[ZnCl<sub>2</sub>(Me<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> and <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> (where H<sub>2</sub>L<sup><em>t</em>Bu</sup> is 2,6-bis(5-<em>tert</em>-butyl-1<em>H</em>-pyrazol-3-yl)pyridine, Me<sub>2</sub>L<sup><em>t</em>Bu</sup> is 2,6-bis(5-<em>tert</em>-butyl-1-methyl-1<em>H</em>-pyrazol-3-yl)pyridine and H<sub>2</sub>L<sup>CatBiPyrPh</sup> is 1,2-bis((5-phenyl-1<em>H</em>-pyrazol-3-yl)methoxy)benzene) were synthesized and characterized using various spectroscopic techniques, including UV-vis, IR, <sup>1</sup>D (<sup>1</sup>H and <sup>13</sup>C) and 2D (<sup>1</sup>H–<sup>1</sup>H COSY) NMR. The structures of complexes <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> and <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> were elucidated through X-ray crystallography. The interactions of the complexes with CT-DNA and human serum albumin (HSA) were investigated using UV-vis spectroscopy and fluorescence emission titration. All examined complexes exhibited quenching constant, <em>K</em><sub>sv</sub>, values in the order of 10<sup>4</sup> with CT-DNA. Constant values followed the trend <strong>[ZnCl<sub>2</sub>(Me<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> < <strong>[Zn<sub>2</sub>Cl<sub>4</sub>(H<sub>2</sub>L<sup>CatBiPyPh</sup>)<sub>2</sub>]</strong> < <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>. The results indicated a moderate interaction between the complexes and HSA. In terms of cytotoxic activity, the zinc(II) complexes significantly decreased the viability of colon (HCT-116) and pancreatic (MIA PaCa-2) cancer cell lines, where the effect on pancreatic cells after 72 h is especially emphasized. The most pronounced occurrence of apoptosis, as the dominant type of complex-induced cell death, was associated with complex <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong>, while necrosis was observed at lower percentages in all investigated treatments. All complexes demonstrated downregulation of the tumor suppressor gene <em>TP53</em> (<em>homo sapiens</em> tumor protein p53). Treatment with <strong>[ZnCl<sub>2</sub>(H<sub>2</sub>L<sup><em>t</em>Bu</sup>)]</strong> resulted in downregulation of <em>TP53</em>, <em>CASP3</em> (<em>Caspase 3</em>) and <em>IGF1R</em> (insulin-like growth factor 1), potentially impairing the effective apoptotic process and reducing cell proliferation.</p> </div> </div> |
| title | New bis-pyrazolate zinc(ii) complexes as potential anticancer drugs: from structure to anticancer activity |
| topic | anticancer activity anticancer drugs spectroscopic techniques |
| url | https://doi.org/10.1039/D5NJ00043B |