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Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2013.01.025

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

Publication TypeJournal Article
Year of Publication2013
AuthorsGermain, AR, Carmody, LC, Nag, PP, Morgan, B, VerPlank, L, Fernandez, C, Donckele, E, Feng, Y, Perez, JR, Dandapani, S, Palmer, M, Lander, ES, Gupta, PB, Schreiber, SL, Munoz, B
JournalBioorg Med Chem Lett
Date Published2013 Mar 15
KeywordsAmides, Breast Neoplasms, Cell Line, Tumor, Drug Screening Assays, Antitumor, Female, Humans, Neoplastic Stem Cells, Small Molecule Libraries, Structure-Activity Relationship

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.


Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID23403082
Grant List1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States