Synthesis and cytotoxicity of new 2-oxo-7-phenyl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid amides |
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| Authors: | Andrii Lozynskyi Borys Zimenkovsky Iryna Ivasechko Julia Senkiv Andrzej Gzella Olexandr Karpenko |
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| Affiliation: | 1. Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Lviv, Ukraine;2. Institute of Cell Biology NAS of Ukraine, Lviv, Ukraine;3. Department of Organic Chemistry, Poznan University of Medical Sciences, Poznan, Poland;4. Enamine Ltd, Kiev, Ukraine |
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| Abstract: | ![]()
AbstractThe synthesis and anticancer activity evaluation of new thiazolo[4,5-b]pyridine-5-carboxylic acid amides is described. The structures of the synthesized compounds were confirmed by spectroscopic data and a single crystal X-ray diffraction analysis for 2.4. The synthesized compounds were screened for their in vitro anticancer activity according to US NCI protocols. The most active 7-(4-fluorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.2 and 7-(4-chlorophenyl)-2-oxo-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (4-chlorophenyl)amide 2.5 were screened for their cytotoxicity effects on C6 Rat glioma cells and U373 Human glioblastoma astrocytoma cells which revealed promising results comparable to temozolamide as reference control according MTT assay data. |
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| Keywords: | 2-oxo-4-phenyl-but-3-enoic acids thiazolo[4,5-b]pyridin-2(3H)-one X-ray study anticancer activity cell lines |
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