title: Selective Inhibition of Bacterial Topoisomerase I by alkynyl-bisbenzimidazoles.
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.
authors.affiliation: Department of Chemistry, Clemson University, Clemson, South Carolina, Unite States 29634.
authors.forename: Nihar
authors.initials: N
authors.lastname: Ranjan
authors.affiliation: Department of Chemistry and Biochemistry, Florida International University, Miami, Florida 33199 (Unite States).
authors.forename: Geraldine
authors.initials: G
authors.lastname: Fulcrand
authors.affiliation: NUBAD, LLC, 900 B West Faris Road, Greenville, South Carolina 29605.
authors.forename: Ada
authors.initials: A
authors.lastname: King
authors.affiliation: Department of Biological Sciences, Clemson University, Clemson, South Carolina 29634.
authors.forename: Joseph
authors.initials: J
authors.lastname: Brown
authors.affiliation: Department of Biological Sciences, Clemson University, Clemson, South Carolina 29634.
authors.forename: Xiuping
authors.initials: X
authors.lastname: Jiang
authors.affiliation: Department of Chemistry and Biochemistry, Florida International University, Miami, Florida 33199 (Unite States).
authors.forename: Fenfei
authors.initials: F
authors.lastname: Leng
authors.affiliation: Department of Chemistry, Clemson University, Clemson, South Carolina, Unite States 29634 ; NUBAD, LLC, 900 B West Faris Road, Greenville, South Carolina 29605.
authors.forename: Dev P
authors.initials: DP
authors.lastname: Arya
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