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

详细信息	查看全文 | 推荐本文 |

• 作者：Andrew R. Germain^a ; Leigh C. Carmody^a ; Barbara Morgan^a ; Cristina Fernandez^a ; Erin Forbeck^a ; Timothy A. Lewis^a ; Partha P. Nag^a ; Amal Ting^a ; Lynn VerPlank^a ; Yuxiong Feng^b ; Jose R. Perez^a ; Sivaraman Dandapani^a ; Michelle Palmer^a ; Eric S. Lander^a ; Piyush B. Gupta^b ; ^c ; Stuart L. Schreiber^a ; ^d ; Benito Munoz^a ; ^{bmunoz@broadinstitute.org} ; ^{benmz101@yahoo.com}
• 关键词：Cancer stem cells ; Breast cancer ; Molecular libraries probe production center ; Network (MLPCN)
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 May, 2012
• 卷：22
• 期：10
• 页码：3571-3574
• 文件大小：1649 K

摘要

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).