作者
Aastha Singh, Kaneez Fatima, Ankita Srivastava, Sadiya Khwaja, Dev Priya, Arjun Singh, Girish Mahajan, Sarfaraz Alam, Ajit K Saxena, DM Mondhe, Suaib Luqman, Debabrata Chanda, Feroz Khan, Arvind S Negi
发表日期
2016/11
来源
Chemical biology & drug design
卷号
88
期号
5
页码范围
625-634
简介
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 (IC50=3–10 μm) against several human cancer cell lines through microtubule destabilization (IC50=1.54 μm) after occupying colchicine‐binding site of β‐tubulin. In cell cycle analysis, compound 8 exerted G2/M phase arrest in both MCF‐7 and MDA‐MB‐231 cells and induced apoptosis. It reduced 34.8% solid tumor in in vivo Ehrlich ascite carcinoma in Swiss albino mice at 30 mg/kg dose. In acute oral toxicity experiment, it was tolerable up to 300 mg/kg doses in Swiss albino mice. The lead compound 8 needs to be optimized for better activity.
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A Singh, K Fatima, A Srivastava, S Khwaja, D Priya… - Chemical biology & drug design, 2016