Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 7, Pages 1651-1659Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.01.029
Keywords
Anticancer agents; Cancer treatment; Complexation studies; Hydrazone; Troger's base
Funding
- Ministry of Education, Youth and Sport of the Czech Republic by the European Social Fund [CZ.1.07/2.3.00/30.0060]
- program NPU [I LO1304]
- Grant Agency of the Czech Republic [GAP303/11/1291]
- Technology Agency of the Czech Republic [TE01020028]
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We report the design and synthesis of novel anticancer agents based on bis-hydrazones separated by a rigid Troger's base skeleton. This novel approach combines a biologically active moiety (hydrazone) with this scaffold (Troger's base) to construct DNA intercalators. Evaluation of the anticancer activity of these agents using seven cancer cell lines and two healthy cell lines found that several derivatives had potent anticancer activity and excellent selectivity indexes toward cancer cells. The antimicrobial activities were tested on a set of thirteen bacterial stains, but the prepared compounds were not active. Complexation studies using biologically important metal ions demonstrated that these compounds are able to bind Cu2+, Fe3+, Co2+, Ni2+ and Zn2+. DNA intercalation studies showed that the compounds themselves do not interact with DNA, but their metallocomplexes do interact, most likely via intercalation into DNA. (C) 2015 Published by Elsevier Ltd.
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