Biopolym. Cell. 2010; 26(6):508-511.
http://dx.doi.org/10.7124/bc.00017B
Bioorganic Chemistry
Inhibition of in vitro transcription by 2-arylidene derivatives of thiazolo[3,2-α]benzimidazol-3(2H)-one
1Palchykovska L. G., 1Alexeeva I. V., 1Negrutska V. V., 1Kostyuk Yu. K., 1Indychenko T. M., 1Kostenko O. M., 1Kryvorotenko D. V., 1Shved A. D., 1Dubey I. Ya.
  1. Institute of Molecular Biology and Genetics, NAS of Ukraine
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03680

Abstract

Aim. To evaluate a series of 2-substituted thiazolo[3,2-α]benzimidazolones as potential transcription inhibitors. Methods. Compounds were tested in a model transcription system based on T7 RNA polymerase. Results. The testing revealed a number of compounds able to inhibit transcription at micromolar concentrations. The most active inhibitor was dihydroxy derivative BT29 with IC50 = 1.6 μM. Conclusions. Structure-functional dependence of the activity of tested compounds as transcription inhibitors was found. The key structural feature required for their high activity is a presence of hydroxy or dialkylamino group at p- or m-position of arylidene fragment.
Keywords: thiazolo[3,2-α]benzimidazolones, transcription inhibitors, T7 RNA polymerase
Full text: (PDF, in English)

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