Table 2. Activity of THIQ Derivative 9c as an Inhibitor of Tubulin Polymerization and Colchicine Binding to Tubulina.
inhibition of colchicine binding |
|||
---|---|---|---|
inhibition of tubulin assembly | % inhibition
± SD |
||
compd | IC50 (μM) ± SD | 5 μM | 50 μM |
CA-4 | 1.3 ± 0.1 | 98 ± 0.6 | |
12a | 2.5 ± 0.1 | 24.5 ± 5 | 74 ± 4 |
12b | 1.3 ± 0.1 | 78 ± 0.9 | |
9c | 15 ± 1 | 13 ± 2 | 59 ± 2 |
Data for 12b are taken from ref (8).