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

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

Author information

1
Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.

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.

PMID:
23403082
DOI:
10.1016/j.bmcl.2013.01.025
[Indexed for MEDLINE]

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