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

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.
Andrew R Germain 1,  Leigh C Carmody,  Partha P Nag,  Barbara Morgan,  Lynn Verplank,  Cristina Fernandez,  Etienne Donckele,  Yuxiong Feng,  Jose R Perez,  Sivaraman Dandapani,  Michelle Palmer,  Eric S Lander,  Piyush B Gupta,  Stuart L Schreiber,  Benito Munoz
Affiliations

Affiliation

  • 1 Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
PMID: 23403082 DOI: 10.1016/j.bmcl.2013.01.025
Abstract

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.

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