Synthesis and structure–activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors

A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC50 values in the single digit nanomolar range. Binding experiments demonstrated that representative active compounds of this class compete with colchicine for its binding site on tubulin. The syntheses and structure–activity relationship studies for the triazole derivatives are described herein.

Graphical abstractThe synthesis and SAR studies on triazole-containing tubulin inhibitor class are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide