Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells

0455809 - ÚMG 2016 RIV US eng J - Journal Article
Kaplánek, R. - Jakubek, M. - Rak, J. - Kejik, Z. - Havlík, M. - Dolenský, B. - Frydrych, I. - Hajduch, M. - Kolář, M. - Bogdanová, K. - Králová, Jarmila - Dzubak, P. - Král, V.
Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.
Bioorganic Chemistry. Roč. 60, Jun (2015), s. 19-29. ISSN 0045-2068. E-ISSN 1090-2120
Grant - others:GA MŠk(CZ) EE2.3.30.0060; GA MŠk CZ.1.07/2.3.00/30.0041; GA MŠk(CZ) LO1304
Program: EE; LD
Institutional support: RVO:68378050
Keywords : Anticancer agents * Cancer treatment * Caffeine-hydrazones * Leukaemia * Selectivity
Subject RIV: EB - Genetics ; Molecular Biology
Impact factor: 2.252, year: 2015

We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and great selectivity index toward T-lymphoblastic leukaemia cells. In general, hydrazones bearing 2-N-heteroaryl moiety are more active and selective than those with 2-hydroxyaryl moiety. Tested compounds exhibit dose-dependent inhibition of both RNA and DNA synthesis, with some exceptions. Antimicrobial activities were tested on set of twelve bacterial and yeast strains, however prepared compounds were not active, suggesting for a molecular target specific for eukaryotic cells. (C) 2015 Elsevier Inc. All rights reserved.
Permanent Link: http://hdl.handle.net/11104/0256433