Anticancer activity of gallic acid template‐based benzylidene indanone derivative as microtubule destabilizer

Benzylidene indanones have been designed and synthesized from gallic acid, a plant phenolic acid as possible anticancer agent. The best analogue of the series, that is, 3‐(3′,4′,5′‐trimethoxyphenyl)‐4,5,6‐trimethoxy‐2‐(4˝‐nitrobenzylidene)‐indan‐1‐one ( 8 ) exhibited potent cytotoxicity ( IC 50 =3–10 μ m ) against several human cancer cell lines through microtubule destabilization ( IC 50 =1.54 μ m ) after occupying colchicine‐binding site of β‐tubulin. In cell cycle analysis, compound 8 exerted G 2/ M phase arrest in both MCF ‐7 and MDA ‐ MB ‐231 cells and induced apoptosis. It reduced 34.8% solid tumor in in vivo E hrlich ascite carcinoma in S wiss albino mice at 30 mg/kg dose. In acute oral toxicity experiment, it was tolerable up to 300 mg/kg doses in S wiss albino mice. The lead compound 8 needs to be optimized for better activity.