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The design and synthesis of biologically active 3d metal coordination compounds of 4-allylchalcogensemicarbazones and their derivatives


Author: Graur Vasilii
Degree:doctor of chemistry
Speciality: 02.00.01 - Inorganic chemistry
Year:2017
Scientific adviser: Aurelian Gulea
doctor habilitat, professor, Moldova State University
Institution: Moldova State University

Status

The thesis was presented on the 12 April, 2017
Approved by NCAA on the 31 May, 2017

Abstract

Adobe PDF document0.65 Mb / in romanian
Adobe PDF document0.60 Mb / in russian

Thesis

CZU 54-386:546.47’56’72’73’74’:547.497.1:615.28

Adobe PDF document 3.44 Mb / in russian
165 pages


Keywords

coordination compounds, 3d metals, 4-allylchalcogensemicarbazones, 4-allyl-S-methylisothiosemicarbazones, antiproliferative activity, antimicrobial activity, antifungal activity

Summary

The thesis consists of introduction, four chapters, general conclusions and recommendations, 148 references, 5 annexes, 120 pages, 53 figures, 20 schemes, 31 tables. The results are published in 17 scientific publications (4 articles, 12 theses at conferences, 1 patent).

Field of study: Nature Sciences

The aim and the objectives of the thesis. The aim of this thesis consists in determination of the influence on the biological activity of different substituents in the first position of 4-allylthiosemicarbazide, alkylation of sulphur atom, and substitution of sulphur atom by selenium atom; determination of the influence of the nature of central atom, nature of ligands, introduction of amines in the inner sphere on composition, structure, physic-chemical and biological properties of the coordination compounds with these ligands; finding of new substances with selective antiproliferative activity against cancer cells and low toxicity. For achievement of these aims, the following objectives were set: synthesis of different 4-allylchalcogensemicarbazones; alkylation of sulphur atom; synthesis of complexes of some 3d metals with these ligands; introduction of amines in the inner sphere of complexes; determination of composition, structure and biological activity of the synthesized substances.

Novelty and relevance of the study consists in the synthesis of 74 new organic and coordination compounds, determination of the effect of substituents in the first position of thiosemicarbazides, alkylation of sulphur atom and substitution of sulphur by selenium atom, introduction of amines in the inner sphere on the properties of biometal coordination compounds.

Scientific problem solved in this thesis: new inhibitors of cancer cells proliferation with high selective activity and low toxicity were synthesized.

The theoretical importance and potential application value of the work. The list of biologically active organic and coordination compounds was enlarged. The influence of different fragments in their composition on the antimicrobial and antitumor properties was determined.

Implementation of scientific results.It was demonstrated that the synthesized substances manifest selective antiproliferative activity towards cancer cells, antimicrobial and antifungal activities and low cytostatic activity against normal cells.