Dzhus O. Morphofunctional characteristics of transformed cell cultures under the influence of modulators of enzymatic activity

The thesis is devoted to study and compare changes of primary and transformed cell culture under the influenсe of substances with unidirectional action (inhibitors to epidermal growth factor receptor with tyrosine kinases activity) and complex substances which incorporating to the structure of a potential drug two or more pharmacophores (functional groups or structural fragments). As a result we found that N-hydroxy-4-({[(e)-2phenylethenyl]sulfonyl}amino) butan amide shows more pronounced cytotoxic / cytostatic effect on cell culture HeLa, which has the less IC 50 than versus MMP inhibitor (Galardin). A significant change in morphological parameters of MCF-7 and Hela transformed cell cultures which characterized to gain the epithelial cell structure, a significant reduction of nuclear-cytoplasmic ratio and inhibition of aneuploid cells content in primary culture LLC, which indicates that inhibition of proliferative, and increased apoptotic and adhesion parameters in vitro and inhibition of metastasis of inoculated Lewis lung carcinoma in vivo. Instead bimetallic complex demonstrated pronounced antitumor effect in vivo, and maleimide derivative - pronounced cytotoxic / cytostatic and proapoptotic effect in vitro with using Hela, MCF-7 and Colo 205 cell cultures.