Anticancer activity and toxicity profiles of 2-benzylidene indanone lead molecule

3-(3′,4′,5′-Trimethoxyphenyl)-4,5,6-trimethoxy,2-(3″,4″-methylenedioxybenzylidene)-indan-1-one (1) is an optimized anti-cancer lead molecule obtained on modification of gallic acid, a plant phenolic acid. It exhibited potent cytotoxicities (IC50 = 0.010-14.76 μM) against various human carcinoma cells. In cell cycle analysis, benzylidene indanone 1 induced G2/M phase arrest in both MCF-7 and MDA-MB-231 cells. It also induced apoptosis in DU145 cells which was evident by cleavage of PARP. In Ehrlich ascites carcinoma, benzylidene indanone 1 showed 45.48% inhibition of tumour growth at 20 mg/kg dose in Swiss albino mice. Further, in sub-acute toxicity experiment in Swiss-albino mice, it was found to be non-toxic up to 100 mg/kg dose for 28 days. The lead compound benzylidene indanone 1 can further be optimized for better anti-cancer activity.

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