Metal Coordination and Biological Screening of a Schiff Base Derived from 8-Hydroxyquinoline and Benzothiazole
Designing new metallodrugs for anticancer therapy is a driving force in the scientific community. Aiming to contribute to this field, we hereby report the development of a Schiff base (H2L) derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with 2-hydrazinobenzothiazole and its compl...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2022
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| Sorozat: | PHARMACEUTICS
14 No. 12 |
| Tárgyszavak: | |
| doi: | 10.3390/pharmaceutics14122583 |
| mtmt: | 33267453 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/25646 |
| LEADER | 02829nab a2200337 i 4500 | ||
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| 001 | publ25646 | ||
| 005 | 20221129144243.0 | ||
| 008 | 221129s2022 hu o 0|| Angol d | ||
| 022 | |a 1999-4923 | ||
| 024 | 7 | |a 10.3390/pharmaceutics14122583 |2 doi | |
| 024 | 7 | |a 33267453 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a Angol | ||
| 100 | 1 | |a Ribeiro Nádia | |
| 245 | 1 | 0 | |a Metal Coordination and Biological Screening of a Schiff Base Derived from 8-Hydroxyquinoline and Benzothiazole |h [elektronikus dokumentum] / |c Ribeiro Nádia |
| 260 | |c 2022 | ||
| 300 | |a 29 | ||
| 490 | 0 | |a PHARMACEUTICS |v 14 No. 12 | |
| 520 | 3 | |a Designing new metallodrugs for anticancer therapy is a driving force in the scientific community. Aiming to contribute to this field, we hereby report the development of a Schiff base (H2L) derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with 2-hydrazinobenzothiazole and its complexation with transition metal ions. All compounds were characterised by analytical and spectroscopic techniques, which disclosed their structure: [Cu(HL)Cl], [Cu(HL)2], [Ni(HL)(acetate)], [Ni(HL)2], [Ru(HL)Cl(DMSO)], [VO(HL)2] and [Fe(HL)2Cl(H2O)]. Different binding modes were proposed, showing the ligand’s coordination versatility. The ligand proton dissociation constants were determined, and the tested compounds showed high lipophilicity and light sensitivity. The stability of all complexes in aqueous media and their ability to bind to albumin were screened. Based on an antiproliferative in vitro screening, [Ni(HL)(acetate)] and [Ru(HL)Cl(DMSO)] were selected for further studies aiming to investigate their mechanisms of action and therapeutic potential towards colon cancer. The complexes displayed IC50 < 21 μM towards murine (CT-26) and human (HCT-116) colon cancer cell lines. Importantly, both complexes exhibited superior antiproliferative properties compared to the clinically approved 5-fluorouracil. [Ni(HL)(acetate)] induced cell cycle arrest in S phase in CT-26 cells. For [Ru(HL)Cl(DMSO)] this effect was observed in both colon cancer cell lines. Additionally, both compounds significantly inhibited cell migration particularly in the human colon cancer cell line, HCT-116. Overall, the therapeutic potential of both metal complexes was demonstrated. | |
| 650 | 4 | |a Kémiai tudományok | |
| 700 | 0 | 1 | |a Farinha Pedro F. |e aut |
| 700 | 0 | 1 | |a Pinho Jacinta O. |e aut |
| 700 | 0 | 1 | |a Luiz Hugo |e aut |
| 700 | 0 | 1 | |a Mészáros János Péter |e aut |
| 700 | 0 | 1 | |a Galvão Adelino M. |e aut |
| 700 | 0 | 1 | |a Pessoa João Costa |e aut |
| 700 | 0 | 1 | |a Enyedy Éva Anna |e aut |
| 700 | 0 | 2 | |a Pinto Reis Catarina |e aut |
| 700 | 0 | 2 | |a Correia Isabel |e aut |
| 700 | 0 | 2 | |a Gaspar Maria Manuela |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/25646/1/Pharmaceutics_2022_14_2583.pdf |z Dokumentum-elérés |