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Bioorganic & medicinal chemistry letters 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
JournalBioorganic & medicinal chemistry letters
Volume23
Issue6
Pages1834-8
Date Published2013/03/15
ISSN0960-894X
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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(13)00047-4
DOI10.1016/j.bmcl.2013.01.025
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/23403082?dopt=Abstract