Literature DB >> 22503247

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

Andrew R Germain1, Leigh C Carmody, Barbara Morgan, Cristina Fernandez, Erin Forbeck, Timothy A Lewis, Partha P Nag, Amal Ting, Lynn VerPlank, Yuxiong Feng, Jose R Perez, Sivaraman Dandapani, Michelle Palmer, Eric S Lander, Piyush B Gupta, Stuart L Schreiber, Benito Munoz.   

Abstract

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).
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22503247     DOI: 10.1016/j.bmcl.2012.01.035

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  11 in total

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9.  Increased macroH2A1.1 expression correlates with poor survival of triple-negative breast cancer patients.

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10.  Correlating chemical sensitivity and basal gene expression reveals mechanism of action.

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Journal:  Nat Chem Biol       Date:  2015-12-14       Impact factor: 15.040

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