Combining a Ru(II) “Building Block” and Rapid Screening Approach to Identify DNA Structure-Selective “Light Switch” Compounds

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• 作者：Erin Wachter ; Diego Moyá ; Edith C. Glazer
• 刊名：ACS Combinatorial Science
• 出版年：2017
• 出版时间：February 13, 2017
• 年：2017
• 卷：19
• 期：2
• 页码：85-95
• 全文大小：535K
• ISSN：2156-8944

文摘

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.