. Author manuscript; available in PMC: 2016 Oct 22.

Published in final edited form as: J Med Chem. 2015 Oct 7;58(20):7991–8010. doi: 10.1021/acs.jmedchem.5b00805

Table 3.

Inhibition of Tubulin Polymerization and Colchicine Binding by Compounds 5a–f, 8f, 9, 12–22, and CA–4

compd	inhibition of tubulin assembly IC₅₀ ± SD (μM)^a,c	inhibition of colchicine binding inhibition ± SD (%)^b,c
5a	2.9 ± 0.1	11 ± 4
5b	>20	nd
5c	1.3 ± 0.05	20 ± 1
5d	6.6 ± 0.3	nd
5e	0.99 ± 0.1	52 ± 5
5f	0.99 ± 0.1	69 ± 3
8f	2.6 ± 0.2	30 ± 4
9	5.7 ± 0.7	nd
12	0.74 ± 0.07	77 ± 2
13	1.8 ± 0.3	61 ± 1
14	1.2 ± 0.1	40 ± 0.9
15	8.0 ± 0.1	nd
16	>20	nd
18	>20	nd
19 ^d	0.57 ± 0.02	73 ± 0.7
20 ^d	0.58 ± 0.05	77 ± 3
21 ^e	0.75 ± 0.04	75 ± 4
22 ^d	0.90 ± 003	83 ± 0.5
CA-4	1.2 ± 0.1	99 ± 0.06

Inhibition of tubulin polymerization. Tubulin was at 10 μM.

Inhibition of [³H]colchicine binding.

Tubulin and colchicine were at 1 and 5 μM, respectively, and the tested compounds were at 5 μM. nd, not determined.

Reference 7.

Reference 8.