Synthesis, cytotoxicity, <i>in-vitro</i> antibacterial screening and <i>in-silico</i> study of novel thieno[2,3-<i>b</i>]pyridines as potential pim-1 inhibitors
Ahmed E. M. Mekky, Sherif M. H. Sanad, Ahmed Y. Said, Mohamed A. A. Elneairy
Abstract
A 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.