Inhibition of in vitro transcription by 2-arylidene derivatives of thiazolo[3,2-]benzimidazol-3(2H)-one
Aim. To evaluate a series of 2-substituted thiazolo[3,2-]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 M. 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 por m-position of arylidene fragment.