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Gallic acid-based indanone derivatives as anticancer agents

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...

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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.
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creator Saxena, Hari Om
Faridi, Uzma
Srivastava, Suchita
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description 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.
doi_str_mv 10.1016/j.bmcl.2008.06.039
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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
title Gallic acid-based indanone derivatives as anticancer agents
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