Journal
MEDCHEMCOMM
Volume 5, Issue 6, Pages 816-825Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4md00140k
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Funding
- NIH [CA125724, GM100607, 5SC1HD063059-04]
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Hoechst dyes are well known DNA binders that non-selectively inhibit the function of mammalian topoisomerase I and II. Herein, we show that Hoechst 33258 based bisbenzimidazoles (DPA 151-154), containing a terminal alkyne, are effective and selective inhibitors of E. coli topoisomerase I. These bisbenzimidazoles displayed topoisomerase I inhibition much better than Hoechst 33342 or Hoechst 33258 with IC50 values in the range of 2.47-6.63 mu M. Bisbenzimidazoles DPA 151-154 also display selective inhibition of E. coli topoisomerase I over DNA gyrase and human topoisomerases I and II, and effectively inhibit bacterial growth.
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