Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1834-8. doi: 10.1016/j.bmcl.2013.01.025. Epub 2013 Jan 16.


A high-throughput screen (HTS) was conducted against stably propagated cancer stem cell (CSC)-enriched populations using a library of 300,718 compounds from the National Institutes of Health (NIH) Molecular Libraries Small Molecule Repository (MLSMR). A cinnamide analog displayed greater than 20-fold selective inhibition of the breast CSC-like cell line (HMLE_sh_Ecad) over the isogenic control cell line (HMLE_sh_eGFP). Herein, we report structure-activity relationships of this class of cinnamides for selective lethality towards CSC-enriched populations.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amides / chemistry*
  • Amides / toxicity
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • Neoplastic Stem Cells / drug effects
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / toxicity
  • Structure-Activity Relationship


  • Amides
  • Small Molecule Libraries