title: Combining a Ru(II) "Building Block" and Rapid Screening Approach to Identify DNA Structure-Selective "Light Switch" Compounds.
abstract: A chemically reactive Ru(II) "building block", able to undergo condensation reactions with substituted diamines, was utilized to create a small library of luminescent "light switch" dipyrido-[3,2-a:2',3'-c] phenazine (dppz) complexes. The impact of substituent identity, position, and the number of substituents on the light switch effect was investigated. An unbiased, parallel screening approach was used to evaluate the selectivity of the compounds for a variety of different biomolecules, including protein, nucleosides, single stranded DNA, duplex DNA, triplex DNA, and G-quadruplex DNA. Combining these two approaches allowed for the identification of hit molecules that showed different selectivities for biologically relevant DNA structures, particularly triplex and quadruplex DNA.
authors.affiliation: Department of Chemistry, University of Kentucky , 505 Rose Street, Lexingon, Kentucky 40506, United States.
authors.forename: Erin
authors.initials: E
authors.lastname: Wachter
authors.affiliation: Department of Chemistry, University of Kentucky , 505 Rose Street, Lexingon, Kentucky 40506, United States.
authors.forename: Diego
authors.initials: D
authors.lastname: Moyá
authors.affiliation: Department of Chemistry, University of Kentucky , 505 Rose Street, Lexingon, Kentucky 40506, United States.
authors.forename: Edith C
authors.identifier: 0000-0002-0190-7742
authors.initials: EC
authors.lastname: Glazer
mesh_terms: D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry*; D004247:DNA / Q000737:chemistry*; D004277:DNA, Single-Stranded / Q000737:chemistry; D054856:G-Quadruplexes; D049449:Luminescence; D049408:Luminescent Agents / Q000138:chemical synthesis / Q000737:chemistry*; D008163:Luminescent Measurements; D009690:Nucleic Acid Conformation; D010619:Phenazines / Q000138:chemical synthesis / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D056831:Coordination Complexes; D004277:DNA, Single-Stranded; D049408:Luminescent Agents; D010619:Phenazines; C051802:triplex DNA; D012428:Ruthenium; D004247:DNA
keywords: DNA structure-selective; Ru(II); biologically relevant; library; parallel screening; “light switch” compounds