Microtubule-targeting agents impact microtubule dynamics to induce mitotic arrest and tumor cell death. Tubulin is therefore a relevant target for the discovery of new agents acting as tumor neovasculature disruptors. Researchers from Nanjing Keygen Biotech Co. Ltd. have reported on the design and optimization of novel tubulin polymerization inhibitors with antiangiogenesis activity that led to the identification of [I] as the compound.