| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369804 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Andrew R. Germain, 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,