Synthesis and anticancer activity of 2-benzylidene indanones through inhibiting tubulin polymerization

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• 作者：A.P. Prakasham^a ; A.K. Saxena^b ; Suaib Luqman^a ; Debabrata Chanda^a ; Tandeep Kaur^b ; Atul Gupta^a ; D.K. Yadav^a ; C.S. Chanotiya^a ; Karuna Shanker^a ; F. Khan^a ; Arvind S. Negi^a ; ^{arvindcimap@rediffmail.com}
• 关键词：Anticancer ; Indanones ; Gallic acid ; Tubulin polymerization inhibition ; Acute oral toxicity
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 May, 2012
• 卷：20
• 期：9
• 页码：3049-3057
• 文件大小：876 K

摘要

In an attempt to discover a potent and selective anticancer agent, gallic acid has been modified to benzylidene indanones as tubulin polymerization inhibitors. These compounds were evaluated against several human cancer cell lines and also evaluated for inhibition of tubulin polymerase in in vitro assays. Three of the analogues exhibited strong cytotoxicity against human cancer cell lines IC₅₀ = 10-880 nM and also showed tubulin polymerization inhibition (IC₅₀ = 0.62-2.04 渭M). Compound 9j, the best candidate of the series was found to be non-toxic in acute oral toxicity in Swiss-albino mice up to 1000 mg/kg dose.