Table 1. Classification of lead anti-Fli-1 compounds.
Drug classes | Number of drugs | Drug name | Effective dose (μ) IC(50)a |
---|---|---|---|
Cardenolides | 10 | Peruvoside, digitoxin, dihydroouabain, quabain, strophanthidin, proscillaridin A, cymarin, convalatoxin, gitioxin, lanatoside C | 0.165–0.33 |
Calcium ionophores | 5 | Calcimycin, alexidine dihydrochloride, gossypol-acetic acid complex, oligomycin A, thapsigargin | 0.66–1.33 |
Topoisomerase I inhibitors | 1 | Camptothecin | 0.33 |
Protein synthesis inhibitors | 2 | Emetine, anisomycin | 0.165–0.66 |
Chemotherapeutic drugs | 4 | Etoposide, dactinomycin, cycloheximide, puromucine dihydrochloride, | 0.66–2.66 |
Others | 8 | Cedrelone, 5-azacytidine, anthothecol, cephaline, dihydrochloride heptahydrate, helveticoside, deacetoxy-7-oxogedunin, pyrvinion pamoate, cantharidin acid | 0.66–5.62 |
Compound library screening resulted in the identification of six drug classes with the indicated number in each class.
IC(50) was calculated as the lowest drug concentration resulting in a 50% reduction of EWS/Fli-1 luciferase activity. Column 3 displays one example of each inhibitor drug class. Column 4 displays the calculated range of effective dose response for each class.