Synthesis and anticancer activity of some 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines |
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| Authors: | Tomá? Gucky Eva ?ezní?ková Petr D?ubák Marián Hajdúch Vladimír Kry?tof |
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| Affiliation: | (1) Laboratory of Growth Regulators, Faculty of Science, Palack? University and Institute of Experimental Botany ASCR, Šlechtitelů 11, 78371 Olomouc, Czech Republic;(2) Laboratory of Experimental Medicine, Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University and Faculty Hospital in Olomouc, Olomouc, Czech Republic |
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| Abstract: | Abstract The deregulation of cell cycle components in cancer cells has provided a rationale for the development of small molecule inhibitors of cyclin-dependent kinases as novel anticancer drugs. A series of 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines was synthesized and their kinase inhibitory activity and cytotoxicity against several cancer cell lines has been evaluated. Some of the compounds of the series exhibited induction of caspase-dependent cell death and inhibition of cyclin-dependent kinase 2 (CDK2). |
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