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

Publication ,  Journal Article
Emmitte, KA; Adjabeng, GM; Andrews, CW; Alberti, JGB; Bambal, R; Chamberlain, SD; Davis-Ward, RG; Dickson, HD; Hassler, DF; Hornberger, KR ...
Published in: Bioorg Med Chem Lett
March 15, 2009

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.

Duke Scholars

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

March 15, 2009

Volume

19

Issue

6

Start / End Page

1694 / 1697

Location

England

Related Subject Headings

  • Tumor Suppressor Proteins
  • Thiophenes
  • Solubility
  • Proto-Oncogene Proteins
  • Protein Serine-Threonine Kinases
  • Protein Kinase Inhibitors
  • Protein Binding
  • Polo-Like Kinase 1
  • Molecular Conformation
  • Models, Chemical
 

Citation

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MLA
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Emmitte, K. A., Adjabeng, G. M., Andrews, C. W., Alberti, J. G. B., Bambal, R., Chamberlain, S. D., … Cheung, M. (2009). Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg Med Chem Lett, 19(6), 1694–1697. https://doi.org/10.1016/j.bmcl.2009.01.094
Emmitte, Kyle A., George M. Adjabeng, C Webb Andrews, Jennifer G Badiang Alberti, Ramesh Bambal, Stanley D. Chamberlain, Ronda G. Davis-Ward, et al. “Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.Bioorg Med Chem Lett 19, no. 6 (March 15, 2009): 1694–97. https://doi.org/10.1016/j.bmcl.2009.01.094.
Emmitte KA, Adjabeng GM, Andrews CW, Alberti JGB, Bambal R, Chamberlain SD, et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694–7.
Emmitte, Kyle A., et al. “Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.Bioorg Med Chem Lett, vol. 19, no. 6, Mar. 2009, pp. 1694–97. Pubmed, doi:10.1016/j.bmcl.2009.01.094.
Emmitte KA, Adjabeng GM, Andrews CW, Alberti JGB, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA, Nailor KE, Pobanz MA, Smith SC, Sung C-M, Cheung M. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1694–1697.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

March 15, 2009

Volume

19

Issue

6

Start / End Page

1694 / 1697

Location

England

Related Subject Headings

  • Tumor Suppressor Proteins
  • Thiophenes
  • Solubility
  • Proto-Oncogene Proteins
  • Protein Serine-Threonine Kinases
  • Protein Kinase Inhibitors
  • Protein Binding
  • Polo-Like Kinase 1
  • Molecular Conformation
  • Models, Chemical