A Small Molecule with Bridged Carbonyl and Tri‐fluoro‐aceto‐phenone Groups Impedes Microtubule Dynamics and Subsequently Triggers Cancer Cell Apoptosis

We identified a new microtubule targeted small molecule, which showed significant anticancer activity and induced apoptotic death of cancer cells. Precisely the central bridged carbonyl group and trifluoro‐acetophenone group of a bis‐benzothiazole molecule (BBT) interacts with tubulin close to the curcumin site and perturbs microtubule dynamics as well as causes microtubule depolymerization. We observed a significant enhancement of fluorescence while BBT interacts with the tubulin through bridged carbonyl moiety, a similar phenomenon to colchicine. Further, BBT activates tumor‐suppressing bim and p53‐puma axes to inhibit cancer survival. It also shows promising results against a tumor spheroid model. BBT is also capable of tumor regression, which shows that this molecule can serve as a potential template for the design of next‐generation microtubule targeted anticancer drugs.