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

Kyle A. Emmitte, George M. Adjebang, C. Webb Andrews, Jennifer G.Badiang Alberti, Ramesh Bambal, Stanley D. Chamberlain, Ronda G. Davis-Ward, Hamilton D. Dickson, Daniel F. Hassler, Keith R. Hornberger, Jeffrey R. Jackson, Kevin W. Kuntz, Timothy J. Lansing, Robert A. Mook, Kristen E. Nailor, Mark A. Pobanz, Stephon C. Smith, Chiu Mei Sung, Mui Cheung

Research output: Contribution to journalArticle

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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.

Original languageEnglish
Pages (from-to)1694-1697
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number6
DOIs
StatePublished - 15 Mar 2009

Keywords

  • Anti-mitotic
  • Cell cycle inhibitor
  • Polo-like kinase
  • Protein binding
  • Solubility
  • Thiophene

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    Emmitte, K. A., Adjebang, G. M., Andrews, C. W., Alberti, J. G. B., Bambal, R., Chamberlain, S. D., Davis-Ward, R. G., Dickson, H. D., Hassler, D. F., Hornberger, K. R., Jackson, J. R., Kuntz, K. W., Lansing, T. J., Mook, R. A., Nailor, K. E., Pobanz, M. A., Smith, S. C., Sung, C. M., & Cheung, M. (2009). Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorganic and Medicinal Chemistry Letters, 19(6), 1694-1697. https://doi.org/10.1016/j.bmcl.2009.01.094