Synthesis and characterization of new transition metal complexes with diffrent hetero-cylic ligands as possible anticancer agents.

number: 
512
إنجليزية
department: 
Degree: 
Imprint: 
Chemistry
Author: 
Mayada Hadi Al-Kaissi
Supervisor: 
Dr. Ayad Hamza Jassim
Dr.Ameer A. Ameer
year: 
2001

Abstract:

Biomedical inorganic chemistry offers the potential for the design novel therapeutic agents for the treatment of diseases, which are currently intractable. In the review of this work we focus on recent developments relating platinum, palladium, copper, and gold anticancer agents with respect to their structure-activity relationship and the general aspects of anticancer metallo- drug design. seven different ligands have been chosen to prepare and to coordinate with Pt(IV), Pt(II), Au(II), and Cu(II) ions forming mono and di- nuclear complexes. All the prepared compounds were isolate and characterized by studying their physicochemical properties such as C.H.N. and M analysis, vibrational and electric spectra, molar conductivities, and magnetic properties, in addition to mass spectral study for some ligands.The reaction of 5-mercapto-3,4- diamino-l,2,4-triazole (LI) with the named metal ions gave square planar complexes except an octahedral with Pt(IV) ion, all of them have 1:2 M:L ratio. Two schiff-base derivitives for LI complexes were prepared using benzaldehyde and Onitrobenzaldehyde. Cu(II), Au(III), and Pd(II) metal ions react with 3,4,5-triaminol, 2,4-triazole (LII) forming octahedral complexes with the first two ions and square planar with the later. All have 1:2 M:L ratio. Schiff-bases derived from bonzatdehyde of the copper and palladium complexes were prepared. Also dithiocarbamate derivatives were synthesies for these complexes. The resulting dithiocarbemates (LIII) were reacted with Pd(II), Pt(IV), Cu(II), and Co(II) to form binuclear complexes, these include Pd-Pd, Pd-Pt, Pd-Co, Cu-Cu, and Cu-Co, which have octahedral geometry around the second atom in all complexes, which have 1:1 M:M ratio. The third class of ligands were those of dithiooxamide derivatives. This include first dithiooxamide itself (LIV) which gave octahedral structure with Pt(IV) and square planar with Pd(II), Pt(II), and Cu(II) with 1:2 M:L ratio. The second member, which was the benzaldehyde schiff base (LV) of dithiooxamide, gave square planar complexes with Pd(II) and Au(III), and octahedral with Cu(II) and Pt(IV) ions in which M:L ratio was also 1:2. The third member of this class was the O-nitrobenzaldehyde schiff base (LVI) of dithioxamide this gave octahedral complexes with Pt(IV) and Cu(II) in 1:2 M:L ratio. The last derivatives was the cyclic 3,4-dimine-l,4-dithiarine (LVII> which form square planar complexes with Pt(II) and Pd(II) of 1:1 M:L ratio. The formation of all the complexes were studied in ethanol solutior following the mole ratio method. The results of both solid state and solutior studies gave identical results. The antibacterial activity (against Kleb., SatmonilLa, BaciUaus, am Staph.) and antifungal activity (against Candida) were studied for all ligand: and their complexes. The results show great enhancement of activity of the complexes relative to that of their respective ligands. The chemical reactivity of the platinum complexes was evaluated toward Glutathion and DNA bases using thiourea and pyridin as biological models following the molar conductance method in water at 38°C. The ratio of thiourea:pyridin activities were in the range (1.3-2.1), which indicate comparable interaction with Glutathion and DNA, this mean relatively low Glutathion resistance and high DNA binding. The high antimicrobial activities of the synthesesed complexes and low Glutathion resistance accompanied by good DNA binding abilities may be regarded due to the structual changes which are designed in these new compounds.