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 mu M) 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. (C) 2015 Elsevier B.V. All rights reserved.