Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells
Two antimony complexes {[Sb(L<sup>1</sup>)Cl<sub>2</sub>] <b>C1</b> and [Sb(L<sup>2</sup>)Cl<sub>2</sub>] <b>C2</b>} with the thiosemicarbazone ligands {<b>HL<sup>1</sup></b> = 4-(2,4-dimethylphenyl)-1-((...
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MDPI AG
2022-10-01
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| Online Access: | https://www.mdpi.com/2304-6740/10/10/172 |
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| author | Amany Fathy Ahmed B. M. Ibrahim S. Abd Elkhalik Florian Meurer Michael Bodensteiner S. M. Abbas |
| author_facet | Amany Fathy Ahmed B. M. Ibrahim S. Abd Elkhalik Florian Meurer Michael Bodensteiner S. M. Abbas |
| author_sort | Amany Fathy |
| collection | DOAJ |
| description | Two antimony complexes {[Sb(L<sup>1</sup>)Cl<sub>2</sub>] <b>C1</b> and [Sb(L<sup>2</sup>)Cl<sub>2</sub>] <b>C2</b>} with the thiosemicarbazone ligands {<b>HL<sup>1</sup></b> = 4-(2,4-dimethylphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide and <b>HL<sup>2</sup></b> = 4-(2,5-dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide} were introduced. The structures were elucidated on the basis of a CHNS analysis, spectroscopic techniques (UV-Vis and FT-IR), and DMF solution electrical conductivities. Single crystal X-ray diffraction analysis of complex <b>C1</b> assigned the complex pseudo-octahedral geometry and triclinic P-1 space group. Only the ligand <b>HL<sup>1</sup></b> and its derived complex <b>C1</b> displayed antifungal activities against <i>Candida albicans</i> and this activity was enhanced from 10 mm to 21 mm for the respective complex, which is the same activity given by the drug “Amphotericin B”. The ligands <b>HL<sup>1</sup></b> and <b>HL<sup>2</sup></b> gave inhibitions, respectively, of 14 and 10 mm against <i>Staphylococcus aureus</i> and 15 and 10 mm against <i>Escherichia coli</i>; however, complexes <b>C1</b> and <b>C2</b> increased these inhibitions to 36 and 32 mm against <i>Staphylococcus aureus</i> and 35 and 31 mm against <i>Escherichia coli</i> exceeding the activities given by the ampicillin standard (i.e., 21 mm against <i>Staphylococcus aureus</i> and 25 mm against <i>Escherichia coli</i>). Against MCF-7 human breast cancer cells, the IC<sub>50</sub> values of <b>HL<sup>1</sup></b> (68.9 μM) and <b>HL<sup>2</sup></b> (145.4 μM) were notably enhanced to the values of 34.7 and 37.4 μM for both complexes, respectively. Further, the complexes induced less toxicity in normal BHK cells (<b>HL<sup>1</sup></b> (126.6 μM), <b>HL<sup>2</sup></b> (110.6 μM), <b>C1</b> (>210.1 μM), and <b>C2</b> (160.6 μM)). As a comparison, doxorubicin gave an IC<sub>50</sub> value of 9.66 μM against MCF-7 cells and 36.42 μM against BHK cells. |
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| spelling | doaj.art-464c2100a8b04512b870bf13a581fd932023-11-24T00:37:10ZengMDPI AGInorganics2304-67402022-10-01101017210.3390/inorganics10100172Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer CellsAmany Fathy0Ahmed B. M. Ibrahim1S. Abd Elkhalik2Florian Meurer3Michael Bodensteiner4S. M. Abbas5Chemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef 62521, EgyptDepartment of Chemistry, Faculty of Science, Assiut University, Assiut 71516, EgyptChemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef 62521, EgyptFaculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, 93053 Regensburg, GermanyFaculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, 93053 Regensburg, GermanyChemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef 62521, EgyptTwo antimony complexes {[Sb(L<sup>1</sup>)Cl<sub>2</sub>] <b>C1</b> and [Sb(L<sup>2</sup>)Cl<sub>2</sub>] <b>C2</b>} with the thiosemicarbazone ligands {<b>HL<sup>1</sup></b> = 4-(2,4-dimethylphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide and <b>HL<sup>2</sup></b> = 4-(2,5-dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide} were introduced. The structures were elucidated on the basis of a CHNS analysis, spectroscopic techniques (UV-Vis and FT-IR), and DMF solution electrical conductivities. Single crystal X-ray diffraction analysis of complex <b>C1</b> assigned the complex pseudo-octahedral geometry and triclinic P-1 space group. Only the ligand <b>HL<sup>1</sup></b> and its derived complex <b>C1</b> displayed antifungal activities against <i>Candida albicans</i> and this activity was enhanced from 10 mm to 21 mm for the respective complex, which is the same activity given by the drug “Amphotericin B”. The ligands <b>HL<sup>1</sup></b> and <b>HL<sup>2</sup></b> gave inhibitions, respectively, of 14 and 10 mm against <i>Staphylococcus aureus</i> and 15 and 10 mm against <i>Escherichia coli</i>; however, complexes <b>C1</b> and <b>C2</b> increased these inhibitions to 36 and 32 mm against <i>Staphylococcus aureus</i> and 35 and 31 mm against <i>Escherichia coli</i> exceeding the activities given by the ampicillin standard (i.e., 21 mm against <i>Staphylococcus aureus</i> and 25 mm against <i>Escherichia coli</i>). Against MCF-7 human breast cancer cells, the IC<sub>50</sub> values of <b>HL<sup>1</sup></b> (68.9 μM) and <b>HL<sup>2</sup></b> (145.4 μM) were notably enhanced to the values of 34.7 and 37.4 μM for both complexes, respectively. Further, the complexes induced less toxicity in normal BHK cells (<b>HL<sup>1</sup></b> (126.6 μM), <b>HL<sup>2</sup></b> (110.6 μM), <b>C1</b> (>210.1 μM), and <b>C2</b> (160.6 μM)). As a comparison, doxorubicin gave an IC<sub>50</sub> value of 9.66 μM against MCF-7 cells and 36.42 μM against BHK cells.https://www.mdpi.com/2304-6740/10/10/172main group elementpenta-coordinate antimonyX-ray crystal structurebacteriafungicancer |
| spellingShingle | Amany Fathy Ahmed B. M. Ibrahim S. Abd Elkhalik Florian Meurer Michael Bodensteiner S. M. Abbas Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells Inorganics main group element penta-coordinate antimony X-ray crystal structure bacteria fungi cancer |
| title | Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells |
| title_full | Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells |
| title_fullStr | Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells |
| title_full_unstemmed | Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells |
| title_short | Thiosemicarbazones and Derived Antimony Complexes: Synthesis, Structural Analysis, and In Vitro Evaluation against Bacterial, Fungal, and Cancer Cells |
| title_sort | thiosemicarbazones and derived antimony complexes synthesis structural analysis and in vitro evaluation against bacterial fungal and cancer cells |
| topic | main group element penta-coordinate antimony X-ray crystal structure bacteria fungi cancer |
| url | https://www.mdpi.com/2304-6740/10/10/172 |
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