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The Synthesis and Biological Evaluation of N-Substituted 1H-Benzimidazol-2-yl-1H-pyrazole-3,5-diamines
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SYSNO ASEP 0460144 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title The Synthesis and Biological Evaluation of N-Substituted 1H-Benzimidazol-2-yl-1H-pyrazole-3,5-diamines Author(s) Jedinák, L. (CZ)
Kryštof, Vladimír (UEB-Q) RID, ORCID
Cankař, P. (CZ)Source Title Journal of Heterocyclic Chemistry - ISSN 0022-152X
Roč. 53, č. 2 (2016), s. 499-507Number of pages 9 s. Language eng - English Country US - United States Keywords ONE-POT SYNTHESIS ; BENZIMIDAZOLE DERIVATIVES ; EFFICIENT SYNTHESIS Subject RIV CE - Biochemistry Institutional support UEB-Q - RVO:61389030 UT WOS 000373397600022 DOI 10.1002/jhet.2315 Annotation The synthesis of 1H-benzimidazol-2-yl-1H-pyrazole-3,5-diamines has been developed. Synthesized bisheteroaryls contain two privileged medicinal scaffolds, aminopyrazole and benzimidazole, with two diversity positions at N1 of benzimidazole and C3 of pyrazole, respectively. The three-step synthesis includes the Mitsunobu N-alkylation of benzimidazole and subsequent one-pot formation of aminopyrazole involving substitution of methylthio groups with amine and hydrazine followed with final ring closure. Inhibitory activity toward cyclin-dependent kinase 2/cyclin E and cytotoxicity against two cancer cell lines were evaluated for all novel pyrazoles. Two compounds showed modest cyclin-dependent kinase inhibition activity and cytotoxicity against cancer cell lines K562 and MCF7. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2017
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