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

Bioorg Med Chem Lett

Authors	Andrew Germain Leigh Carmody Partha Nag Barbara Morgan Lynn VerPlank Cristina Fernandez Etienne Donckele Yuxiong Feng José Perez Sivaraman Dandapani Michelle Palmer Eric Lander Piyush Gupta Stuart Schreiber Benito Munoz
Keywords	Female Humans Breast Neoplasms Cell Line, Tumor Structure-Activity Relationship Small Molecule Libraries Amides Drug Screening Assays, Antitumor Neoplastic 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.
Year of Publication	2013
Journal	Bioorg Med Chem Lett
Volume	23
Issue	6
Pages	1834-8
Date Published	2013 Mar 15
ISSN	1464-3405
URL	http://linkinghub.elsevier.com/retrieve/pii/S0960-894X(13)00047-4
DOI	10.1016/j.bmcl.2013.01.025
PubMed ID	23403082
Links	DOI Google Scholar PubMed
Grant list	1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States