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Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. | LitMetric

AI Article Synopsis

  • Researchers optimized thiophene PLK1 inhibitors by adding basic amine groups to improve their solubility and lower protein binding.
  • The modifications led to interesting selectivity, distinguishing PLK1 from PLK3.
  • This optimization could enhance the effectiveness of treatments targeting these proteins.

Article Abstract

A series of thiophene PLK1 inhibitors was optimized for increased solubility and reduced protein binding through the appendage of basic amine functionality. Interesting selectivity between PLK1 and PLK3 was also obtained through these modifications.

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Source
http://dx.doi.org/10.1016/j.bmcl.2009.01.094DOI Listing

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