Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
Bioorg Med Chem Lett. 2013 Mar 15;23(6):1834-8. doi: 10.1016/j.bmcl.2013.01.025. Epub 2013 Jan 16.
A high-throughput screen (HTS) was conducted against stably propagated cancer stem cell (CSC)-enriched populations using a library of 300,718 compounds from the National Institutes of Health (NIH) Molecular Libraries Small Molecule Repository (MLSMR). A cinnamide analog displayed greater than 20-fold selective inhibition of the breast CSC-like cell line (HMLE_sh_Ecad) over the isogenic control cell line (HMLE_sh_eGFP). Herein, we report structure-activity relationships of this class of cinnamides for selective lethality towards CSC-enriched populations.
采用来自美国国立卫生研究院（NIH）分子库小分子库（MLSMR）的 300718 种化合物库，对稳定增殖的癌症干细胞（CSC）富集群体进行了高通量筛选（HTS）。一种肉桂酰胺类似物对乳腺 CSC 样细胞系（HMLE_sh_Ecad）的选择性抑制作用大于 20 倍，而对同基因对照细胞系（HMLE_sh_eGFP）则没有。在此，我们报告了这类肉桂酰胺的构效关系，它们对 CSC 富集群体具有选择性致死作用。
