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A synthesis and biological screening of predicted inhibitors of Tyrosine Kinases, e.g. KDR, designed in silico

Abstract : Protein kinases represent a group of enzymes responsible for phosphorylation - transfer of aphosphate group from adenosine triphosphate (ATP) to tyrosine or serine/threonine residues. Protein phosphorylation is one of the most important tools regulating a cell activity. A cell "signalization" through an endothelial receptor tyrosine kinase VEGFR2 TK (KDR) is the important pathway influencing growth of a tumor. Small-molecule inhibitors of VEGFR2 TK (VEGFR2 TKls) have become an important tool for the treatment of various types of cancer. This dissertation thesis resulted in a discovery of 16 biologically active N,5-diaryloxazol-2-amines (IC50, VEGFR2 TK). Very good results were achieved especially with compounds 189, 191, 211, 214, 220, 221, 223 and 4 exhibiting the activity under 500 nM.
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Peter Šramel. A synthesis and biological screening of predicted inhibitors of Tyrosine Kinases, e.g. KDR, designed in silico. Organic chemistry. Université de Strasbourg; Univerzita Komenského (Bratislava), 2017. English. ⟨NNT : 2017STRAF064⟩. ⟨tel-02918015⟩

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