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Creators/Authors contains: "Ye, Zhihan"

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  1. ; ; ; ; ; ; ; (, Chemical Biology & Drug Design)
    Abstract In this paper, we report the synthesis of a phenanthroline and neomycin conjugate (7). Compound7binds to a human telomeric G‐quadruplex (G1) with a higher affinity compared with its parent compounds (phenanthroline and neomycin), which is determined by several biophysical studies. Compound7shows good selectivity for G‐quadruplex (G4) DNA over duplex DNA. The binding of7withG1is predominantly enthalpy‐driven, and the binding stoichiometry of7withG1is one for the tight‐binding event as determined by ESI mass spectrometry. A plausible binding mode is a synergistic effect of end‐stacking and groove interactions, as indicated by docking studies. Compound7can inhibit human telomerase activity at low micromolar concentrations, which is more potent than previously reported 5‐substituted phenanthroline derivatives. 
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