Gallic acid-based indanone derivatives as anticancer agents

• Published in: Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.3914-3918
• Main Authors: Saxena, Hari Om, Faridi, Uzma, Srivastava, Suchita, Kumar, J.K., Darokar, M.P., Luqman, Suaib, Chanotiya, C.S., Krishna, Vinay, Negi, Arvind S., Khanuja, S.P.S.
• Format: Article
• Language: English
• Subjects: Anticancer; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Antioxidants - pharmacology; Biological and medical sciences; Cell Line, Tumor; Chemistry, Pharmaceutical - methods; Drug Design; Drug Screening Assays, Antitumor; Erythrocytes - drug effects; Gallic acid; Gallic Acid - chemistry; General aspects; Hemolysis; HMQC; Humans; Indanones; Indans - chemical synthesis; Indans - chemistry; Inhibitory Concentration 50; Medical sciences; Models, Chemical; Osmosis; Osmotic fragility; Pharmacology. Drug treatments; Tetrazolium Salts - pharmacology; Thiazoles - pharmacology
• ISSN: 0960-894X; 0968-0896; 1464-3405; 1464-3391
• DOI: 10.1016/j.bmcl.2008.06.039

Gallic acid-based indanone derivatives have been synthesised. Indanones 10, 11, 12 and 14 showed potent anticancer activity (IC 50 = 0.022–2.2 μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line ( 10, IC 50 = 2.2 μM) showed no toxicity to human erythrocytes even at higher concentrations (100 μg/ml, 258 μM). While, some of the indanones exhibited toxicity to erythrocytes at higher concentrations. Gallic acid-based indanones may further be optimised as better anticancer agents with low toxicity. Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds 10, 11, 12 and 14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone ( 10, IC 50 = 2.2 μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100 μg/ml, 258 μM). While, indanones 11, 12 and 14 showed toxicities to erythrocytes at higher concentrations.