title: Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
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.
authors: Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
authors: Andrew R
authors: AR
authors: Germain
authors: Leigh C
authors: LC
authors: Carmody
authors: Partha P
authors: PP
authors: Nag
authors: Barbara
authors: B
authors: Morgan
authors: Lynn
authors: L
authors: Verplank
authors: Cristina
authors: C
authors: Fernandez
authors: Etienne
authors: E
authors: Donckele
authors: Yuxiong
authors: Y
authors: Feng
authors: Jose R
authors: JR
authors: Perez
authors: Sivaraman
authors: S
authors: Dandapani
authors: Michelle
authors: M
authors: Palmer
authors: Eric S
authors: ES
authors: Lander
authors: Piyush B
authors: PB
authors: Gupta
authors: Stuart L
authors: SL
authors: Schreiber
authors: Benito
authors: B
authors: Munoz
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000633:toxicity; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D014411:Neoplastic Stem Cells / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D054852:Small Molecule Libraries