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Deanship of Graduate Studies
Document Details
Document Type
:
Thesis
Document Title
:
Synthesis and Anticancer Properties of Platinum and Palladium-containing Tridentate Ligands
تحضير ودراسة الخواص المضادة لسرطان لمعقدات البلاتينيوم والبلاديوم المحتوية على متصلات ثلاثية الإعطاء
Subject
:
Faculty of Science
Document Language
:
Arabic
Abstract
:
The aim of thesis is to study the anticancer properties of platinum and palladium complexes containing tridentate Schiff base ligands. Nine tridentate Schiff base ligands were synthesized from the reaction of {2-picolylamine, N-phenylethylenediamine or N-phenyl-O-phenylenediamine} with salicylaldehyde derivatives. One more ligand was obtained by the reduction of one of the Schiff bases with NaBH4. The obtained ligands employed in synthesizing ten platinum(II) and five palladium(II) complexes with the general formula M(N^N^O)Cl. All the compounds were characterized by 1H, 13C NMR and mass spectrometry. X-ray single crystal structures were obtained for (four) ligands and two complexes. The DNA-binding behaviour of the metal complexes were studies by two techniques. Seven of the platinum(II) complexes are believed to initially bind by intercalation followed by switching to covalent binding mode with the DNA. The other platinum(II) and the palladium(II) complexes exhibit faster covalent binding to ct-DNA as estimated by changes in the DNA viscosity by the binding compounds. Binding of the complexes to bovine serum albumin (BSA) was investigated, revealing the formation of complex-BSA adducts as suggested by the static quenching process of the fluorescent BSA. The results of the anticancer screening by MTT assay suggested that platinum(II) complexes with ligand derived from N-phenyl-o-phenylenediamine or 2-picolylamine with 3-ethyoxy-salicyadehyde (Pt-PhN-OEt and Pt-Py-OEt) have the best IC50 values (6.99 and 10.15μM )respectively against HepG2–10.97 and 13.27μM respectively against MCF-7); they have IC50 values less than that for cisplatin (19.73 μM against HepG2 - 18.36 μM against MCF-7). Cell cycle arrest studies suggested that the two platinum(II) complexes activate apoptotic cell death but via a different mechanism from that of cisplatin. On the other hand, the results of the anticancer screening by MTT assay suggested that palladium(II) complexes with ligand derived from 2-picolylamine with 3- ethyoxy-salicyadehyde or 4-diethylamino-salicyadehyde (Pd-Py-OEt and Pd-Py-NEt2 ) have the best IC50 values (18.30 and 20.90) μM respectively against HepG2- (20.30 and 19.66) μM respectively against MCF-7; they have IC50 values comparable to that of cisplatin. Cell cycle arrest studies suggested that the two palladium(II) complexes activate apoptotic cell death but via a different mechanism from that of cisplatin
Supervisor
:
Prof. Dr. Bandar Abdullah Babgi
Thesis Type
:
Doctorate Thesis
Publishing Year
:
1445 AH
2023 AD
Added Date
:
Tuesday, October 31, 2023
Researchers
Researcher Name (Arabic)
Researcher Name (English)
Researcher Type
Dr Grade
Email
كامله صالح الراشدي
Alrashdi, Kamelah Saleh
Researcher
Doctorate
Files
File Name
Type
Description
49467.pdf
pdf
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