Enhancing the anticancer properties of cardiac glycosides by neoglycorandomization - PubMed (original) (raw)

Summary of IC50 data from the high-throughput cytotoxicity assay. Reciprocal IC50 values are displayed for clarity, with the current illustration representing an IC50 range of 18 nM (5β, HCT-116) to >25 μM (e.g., 35β, all cell lines). In the assay, live cells were distinguished by the presence of a ubiquitous intracellular enzymatic activity that converts the nonfluorescent cell-permeant molecule calcein AM to the intensely fluorescent molecule calcein, which is retained within live cells. The IC50 value for each library member represents at least six replicates of dose–response experiments conducted over five concentrations at 2-fold dilutions. For the entire panel of 81 compounds in 10 cell lines, the average error was 17%. IC50 values and corresponding error values can be found in Tables 4 and 5, which are published as

supporting information

on the PNAS web site. The six library member “hits” are depicted in pyranose 4C1 conformations to facilitate structural comparisons. Du145, human colon carcinoma; MCF7, human breast carcinoma; HCT-116, human colon carcinoma; Hep3B, human liver carcinoma; SF-268, human CNS glioblastoma; SK-OV-3, human ovary adenocarcinoma; NCI-H460, human lung carcinoma; A549, human lung adenocarcinoma; NCI/ADR-RES, human breast carcinoma; NmuMG, mouse mammary normal epithelial cells.