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Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2012.01.035

Identification of a selective small molecule inhibitor of breast cancer stem cells.

Publication TypeJournal Article
Year of Publication2012
AuthorsGermain, AR, Carmody, LC, Morgan, B, Fernandez, C, Forbeck, E, Lewis, TA, Nag, PP, Ting, A, VerPlank, L, Feng, Y, Perez, JR, Dandapani, S, Palmer, M, Lander, ES, Gupta, PB, Schreiber, SL, Munoz, B
JournalBioorg Med Chem Lett
Date Published2012 May 15
KeywordsBreast Neoplasms, Female, Humans, Hydrazones, Neoplastic Stem Cells, Pyrroles

A high-throughput screen (HTS) with the National Institute of Health-Molecular Libraries Small Molecule Repository (NIH-MLSMR) compound collection identified a class of acyl hydrazones to be selectively lethal to breast cancer stem cell (CSC) enriched populations. Medicinal chemistry efforts were undertaken to optimize potency and selectivity of this class of compounds. The optimized compound was declared as a probe (ML239) with the NIH Molecular Libraries Program and displayed greater than 20-fold selective inhibition of the breast CSC-like cell line (HMLE_sh_Ecad) over the isogenic control line (HMLE_sh_GFP).


Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID22503247
Grant List1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States