Triaminotriazine DNA helicase inhibitors with antibacterial activity

…, R Reddy, F Arhin, A Belley, D Lehoux, G Moeck…

Index: McKay, Geoffrey A.; Reddy, Ranga; Arhin, Francis; Belley, Adam; Lehoux, Dario; Moeck, Greg; Sarmiento, Ingrid; Parr, Thomas R.; Gros, Philippe; Pelletier, Jerry; Far, Adel Rafai Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 5 p. 1286 - 1290

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Citation Number: 40

Abstract

Screening of a chemical library in a DNA helicase assay involving the Pseudomonas aeruginosa DnaB helicase provided a triaminotriazine inhibitor with good antibacterial activity but associated cytotoxicity toward mammalian cells. Synthesis of analogs provided a few inhibitors that retained antibacterial activity and demonstrated a significant reduction in cytotoxicity. The impact of serum and initial investigations toward a mode of action ...