Biopolym. Cell. 2016; 32(6):468-471.
http://dx.doi.org/10.7124/bc.00093E
Short Communications
Telomerase inhibition by new di- and trisubstituted acridine derivatives
1Negrutska V. V., 1Saraieva I. V., 1Kostina V. G., 1Alexeeva I. V., 1Lysenko N. A., 1Dubey I. Ya.
  1. Institute of Molecular Biology and Genetics, NAS of Ukraine
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03680

Abstract

Aim. To study a series of new acridine derivatives containing two basic fragments able to bind to quadruplex DNA at C-4 and C-9 positions as potential telomerase inhibitors. Methods. TRAP assay was used to determine the activity of compounds in vitro. Results. A number of acridines inhibiting the enzyme at micromolar concentrations were found, with IC50 = 2.6 µM for the most active compound. Conclusions. The introduction of a highly basic N,N-dimethylaminoalkyl group at the C-9 position of the acridine core results in a strong increase of biological activity of compounds, and a 5-methyl substituent further enhances it.
Keywords: telomerase inhibitors, acridines, quadruplex DNA, TRAP
Full text: (PDF, in English)

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