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. Author manuscript; available in PMC: 2014 Sep 1.
Published in final edited form as: Eur J Med Chem. 2013 Jun 29;67:196–207. doi: 10.1016/j.ejmech.2013.06.041

Table 3.

Inhibition of tubulin polymerizationa and colchicine binding to tubulinb

Compound Inhibition of tubulin assembly
IC50 (μM) ± SD		 Inhibition of colchicine binding
(%) inhibition ± SD
at 5 μM at 1 μM
4f 2.2 ± 0.2 71 ± 0.3 NDc
4i 1.6 ± 0.04 69 ± 3.0 ND
5f 1.0 ± 0.1 75 ± 1.0 ND
6b 1.0 ± 0.1 87 ± 2.0 61 ± 2.0
6c 1.0 ± 0.1 98 ± 0.2 89 ± 2.0
6d 0.93 ± 0.04 99 ± 0.6 95 ± 0.7
6e 0.92 ± 0.06 95 ± 0.2 76 ± 0.1
CA4 d 0.96 ± 0.07 98 ± 0.6 90 ± 0.2
a

The tubulin assembly assay measured the extent of assembly of 10 μM tubulin after 20 min at 30 °C.

b

Tubulin: 1 μM. [3H]colchicine: 5 μM. Inhibitor: 5 μM or 1 μM (compounds inhibiting colchicine binding by more than 80% at 5 μM were further tested). Incubation was performed for 10 min at 37 °C.

c

Not determined.

d

reference compound is a drug candidate in phase II/III clinical trials.