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

Bioorg Med Chem Lett
Authors
Keywords
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).

Year of Publication
2012
Journal
Bioorg Med Chem Lett
Volume
22
Issue
10
Pages
3571-4
Date Published
2012 May 15
ISSN
1464-3405
URL
DOI
10.1016/j.bmcl.2012.01.035
PubMed ID
22503247
Links
Grant list
1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States