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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • 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

Published Date

  • March 15, 2009

Published In

Volume / Issue

  • 19 / 6

Start / End Page

  • 1694 - 1697

PubMed ID

  • 19237286

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2009.01.094


  • eng

Conference Location

  • England