Journal
MONATSHEFTE FUR CHEMIE
Volume 141, Issue 6, Pages 709-714Publisher
SPRINGER WIEN
DOI: 10.1007/s00706-010-0314-4
Keywords
Pyrazolo[4,3-e][1,2,4]triazine; Anticancer; Cyclin-dependent kinase; Inhibitor; Caspase; Apoptosis
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Funding
- Ministry of Education, Youth and Sports [MSM6198959216]
- Czech Science Foundation [204/08/0511, 301/08/1649]
- EEA/Norway Financial Mechanisms [CZ0099]
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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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