Synthesis and Biological Evaluation of Some New Thieno[2,3-b]pyridine-based Compounds As Antimicrobial and Anticancer Agents

Document Type : Original Article


Therapeutic Chemistry Department, National Research Centre, Cairo, Egypt.



The risk elicited by the evolution of antimicrobial resistance, in addition to the annual increase in cancer rates, constitute the greatest threat to global health, which led to an urgent need to discover new molecules having potent antimicrobial and anticancer properties. Therefore, the present study involved with the synthesis of some new thieno[2,3-b]pyridine-based compounds 3a-c–6a,b via treatment of the starting 3-aminothienopyridine derivatives 2a,b with aryl isothiocyanates, maleic anhydride and cyclopentanone to afford the target 3-substituted-thienopyridine compounds 3a-c–5a,b. Also, the synthetic target cyclopentapyrido-thienopyridine-9-amines 6a,b were obtained upon treatment of the new 3-cyclopentylideneamino derivatives with phosphorous oxychloride. All the target compounds were evaluated for their in vitro antimicrobial activity against a panel of five bacterial and five fungal strains. Also, the cytotoxic potency of the target compounds was evaluated against two human cancer cell lines; hepatocellular carcinoma (HepG-2) and breast cancer cells (MCF-7). The new compounds showed promising antimicrobial and anticancer activities compared with the reference drugs. The most potent antimicrobial activity was revealed by 3c with MIC values range 4-16 μg/mL. While, the most potent cytotoxicity against both HepG-2 and MCF-7 cells was showed by 4b with IC50 values 3.12 µM and 20.55 µM, respectively.


Main Subjects