Title: Inhibition of in vitro transcription by 2-arylidene derivatives of thiazolo[3,2-α]benzimidazol-3(2H)-one.
Authors: Palchykovska, L. G.; Alexeeva, I. V.; Negrutska, V. V.; Kostyuk, Yu. K.; Indychenko, T. M.; Kostenko, O. M.; Kryvorotenko, D. V.; Shved, A. D.; Dubey, I. Ya.
Abstract: Aim. To evaluate a series of 2-substituted thiazolo[3,2-a]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 mM. 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.
Subjects: BENZIMIDAZOLES; RNA polymerases; ENTEROVIRUSES; BENZODIAZEPINES; NUCLEIC acid synthesis
Publication: Biopolymers & Cell, 2010, Vol 26, Issue 6, p508
ISSN: 0233-7657
Publication type: Academic Journal
DOI: 10.7124/bc.00017B

Inhibition of in vitro transcription by 2-arylidene derivatives of thiazolo[3,2-α]benzimidazol-3(2H)-one.

Palchykovska, L. G.; Alexeeva, I. V.; Negrutska, V. V.; Kostyuk, Yu. K.; Indychenko, T. M.; Kostenko, O. M.; Kryvorotenko, D. V.; Shved, A. D.; Dubey, I. Ya.