Synthesis,cytotoxicity, in-vitro antibacterial screening and in-silico study of novel thieno[2,3-b]pyridines as potential pim-1 inhibitors |
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Authors: | Ahmed E. M. Mekky Ahmed Y. Said Mohamed A. A. Elneairy |
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Affiliation: | 1. Chemistry Department, Faculty of Science, Cairo University, Giza, Egypthttps://orcid.org/0000-0002-8226-010X;2. Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt |
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Abstract: | AbstractA novel series of thieno[2,3-b]pyridines was prepared via an one-step protocol in excellent yields. The protocol involved the reaction of pyridine-2(1H)-thiones with the appropriate halogen containing reagents in ethanolic sodium ethoxide solution under stirring at 80?°C for 2?h. The new thienopyridines were screened against different bacterial and fungal strains. Thieno[2,3-b]pyridine-2-carboxylate 9a showed the most effective antibacterial activities against each of Staphylococcus aureus and Escherichia coli with MIC/MBC values of 9.9/19.8 and 19.8/39.5?µM, respectively, when compared with Ciprofloxacin. 9a was the most effective compound against MRSA with inhibition zone of 16.2?±?0.6?mm, when compared with Gentamicin. Moreover, 9a exhibited the best cytotoxic activity against each of HEPG2 and MCF-7 cell lines with IC50 values of 25.7 and 30.53?µM, respectively, when compared with Doxorubicin. The in-silico study was performed to predict the capability of new thienopyridines as potential inhibitors of pim-1 kinase. |
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Keywords: | In-silico study in-vitro antimicrobial activity pim-1 inhibitors pyridine-2(1H)-thione thieno[23-b]pyridine |
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