Table 4.
Bioassay Data for Compounds in this Study.
| cmpd. | NSC # | GI50 (μM) | Cell-based microfilament assayb | ||||||
|---|---|---|---|---|---|---|---|---|---|
| HCT-116a | MDA-MB-231a | 0.01 μM | 0.05 μM | 0.1 μM | 0.5 μM | 1.0 μM | 5.0 μM | ||
| 1 | 613009 | 0.04 | 0.01 | - | - | - | +++ | +++ | +++ |
| 3 | 731258 | 0.14c | 0.04 | - | + | + | ++ | ++ | ++ |
| 4 | 751841 | 0.02 | 0.02 | NT | |||||
| 5 | 751842 | 0.11 | 0.26 | NT | |||||
| 6 | 751843 | 0.13 | 0.21 | NT | |||||
| 7 | 751844 | 0.05 | 0.07 | NT | |||||
| 8 | 751837 | 0.06 | 0.09 | - | - | - | +++ | +++ | +++ |
| 9 | 666654 | 13.7c | 2.50 | - | - | - | - | - | - |
| 10 | –d | 0.27c | NT | - | - | - | + | ++ | ++ |
| 11 | 751840 | 0.28c | 0.74 | - | - | - | + | ++ | ++ |
| 12 | 751838 | 11.1 | 22.3 | - | - | - | - | - | - |
| 13 | 751839 | 0.07 | 0.09 | - | + | ++ | +++ | +++ | +++ |
| 14 | 662466 | 3.84 | 2.32 | - | - | - | - | - | - |
| 15 | 752380 | NAe | NA | - | - | - | - | - | - |
a
GI50 data provided by the National Cancer Institute-Developmental Therapeutics Program (NCI-DTP). For the comprehensive data set against 60 cell lines use the NSCs above at http://dtp.nci.nih.gov/.
b
The microfilament-disrupting effects were evaluated based on image analysis of the actin cytoskeleton in fixed HCT-116 cells: (+) Loss of microfilament; (++) Additional loss of microfilament; (+++) Total loss of microfilament network; (-) inactive.
c
IC50 determined by the Valeriote group at Henry Ford Hospital.
d
10 was not selected for testing by the NCI-DTP.
e
15 displayed < 25% growth inhibition at 10 μM and was not selected for five-dose testing. NT=not tested, NA=not active.