. 2022 Nov 17;65(23):15805–15818. doi: 10.1021/acs.jmedchem.2c01457

Table 1. Inhibition of Tubulin Polymerization, Inhibition of the Growth of MCF-7 Human Breast Carcinoma Cells by Compounds 2–16, and Inhibition of the Binding of Colchicine to Tubulin^a.

Experiments were performed in duplicate or triplicate.

Inhibition of tubulin polymerization. Tubulin was at 10 μM in the assembly assay. CSA4 as a reference compound yielded IC₅₀s in the 0.54–0.73 mM range.

Inhibition of the growth of MCF-7 human breast carcinoma cells.

Inhibition of [³H]colchicine binding: tubulin, [³H]colchicine, inhibitor at 1:5:5 μM.

Inhibition of [³H]colchicine binding: tubulin, [³H]colchicine, inhibitor at 1:5:1 μM: 6, 69 ± 1%; 9, 66 ± 2%. Inhibition of colchicine binding by CSA4: 98% at 5 μM, 78% at 1 μM.

Table 1. Inhibition of Tubulin Polymerization, Inhibition of the Growth of MCF-7 Human Breast Carcinoma Cells by Compounds 2–16, and Inhibition of the Binding of Colchicine to Tubulina.

Table 1. Inhibition of Tubulin Polymerization, Inhibition of the Growth of MCF-7 Human Breast Carcinoma Cells by Compounds 2–16, and Inhibition of the Binding of Colchicine to Tubulin^a.