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Synthesis and anticancer activity evaluation of 3-(4-oxo-2-thioxothiazolidin-5-yl)-1H-indole-carboxylic acids derivatives |
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| Authors: | Anna Kryshchyshyn-Dylevych Myroslav Garazd Andrew Karkhut Sviatoslav Polovkovych |
| Institution: | 1. Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Lviv, Ukraine;2. Eximed, Kyiv, Ukraine;3. Department of Technology of Biologically Active Substances, Pharmacy and Biotechnology, Lviv Polytechnic National University, Lviv, Ukraine |
| Abstract: | AbstractA mild and efficient method for the synthesis of 1-oxo-9H-thiopyrano3,4-b]indole-3-carboxylic acids and dimerized 3-(4-carboxy-1H-3-indolyl)-2-propenoic acids via alkaline hydrolysis of 3-(rhodanin-5-yl)-1H-indole-2-carboxylic acids derivatives was elaborated. Anticancer activity screening in NCI60-cell lines assay allowed identification of 5-fluoro-3-(4-oxo-2-thioxothiazolidin-5-ylidenemethyl)-1H-indole-2-carboxylic acid methyl ester 2a with significant antimitotic activity at micromolar and submicromolar concentrations. |
| Keywords: | Anticancer activity indoles Knoevenagel reaction ring transformations 2-thioxo-4-thiazolidinones |