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Issue 6, 2014
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Selective inhibition of bacterial topoisomerase I by alkynyl-bisbenzimidazoles

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Abstract

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 μM. 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.

Graphical abstract: Selective inhibition of bacterial topoisomerase I by alkynyl-bisbenzimidazoles

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Publication details

The article was received on 25 Mar 2014, accepted on 24 Apr 2014 and first published on 25 Apr 2014


Article type: Concise Article
DOI: 10.1039/C4MD00140K
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Med. Chem. Commun., 2014,5, 816-825

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    Selective inhibition of bacterial topoisomerase I by alkynyl-bisbenzimidazoles

    N. Ranjan, G. Fulcrand, A. King, J. Brown, X. Jiang, F. Leng and D. P. Arya, Med. Chem. Commun., 2014, 5, 816
    DOI: 10.1039/C4MD00140K

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