Recent Advances in Synthetic Strategies and Medicinal Properties of Thienopyridines
- 1Translational Medicine Research Center, Sirius University of Science and Technology, Olympic Ave., 1, Sirius 354340, Russia
- 2Department of Physical Organic Chemistry, Institute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya Nab., Saint Petersburg 199034, Russia
Abstract
This review provides an updated overview of recent advances (2024–present) in the synthesis and medicinal applications of thienopyridines and their fused derivatives. Synthetic methodologies are categorized into three strategic approaches: (i) thiophene ring construction onto a preformed pyridine core; (ii) pyridine ring annulation onto a thiophene scaffold—ranging from classical Friedländer and Gould–Jacobs reactions to modern metal-catalyzed, photo-induced, and electrochemical transformations; and (iii) multicomponent reactions for the simultaneous assembly of both heterocyclic rings. Furthermore, the strategic functionalization of preformed thienopyridine scaffolds to access complex tri- and polyheterocyclic systems is discussed. From a biological perspective, the review highlights the scaffold’s expanding therapeutic repertoire, including antibacterial, antifungal, and antiviral activities; potent anticancer applications targeting tumor-associated enzymes and emerging Proteolysis Targeting Chimera (PROTAC)/Deubiquitinase-Targeting Chimera (DUBTAC) technologies; and modulation of neurological, neuropsychiatric, and metabolic disorders. Finally, recent progress in the agrochemical utility of thienopyridines as insecticides and herbicide safeners is examined. Collectively, this work underscores the enduring relevance of the thienopyridine scaffold as a versatile platform for next-generation drug and agrochemical discovery.
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BibTeX
@article{ermolaeva2026recent,
title = {{Recent Advances in Synthetic Strategies and Medicinal Properties of Thienopyridines}},
author = {Anfisa Ermolaeva and Svetlana Baykova and Sergey Baykov and Roman Ivanov and Ekaterina Minskaia},
journal = {International Journal of Molecular Sciences},
year = {2026},
month = oct,
doi = {10.3390/ijms27208962},
url = {https://www.mdpi.com/1422-0067/27/20/8962},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Recent Advances in Synthetic Strategies and Medicinal Properties of Thienopyridines
AU - Anfisa Ermolaeva
AU - Svetlana Baykova
AU - Sergey Baykov
AU - Roman Ivanov
AU - Ekaterina Minskaia
PY - 2026
DA - 2026/10/09
JO - International Journal of Molecular Sciences
DO - 10.3390/ijms27208962
UR - https://www.mdpi.com/1422-0067/27/20/8962
AB - This review provides an updated overview of recent advances (2024–present) in the synthesis and medicinal applications of thienopyridines and their fused derivatives. Synthetic methodologies are categorized into three strategic approaches: (i) thiophene ring construction onto a preformed pyridine core; (ii) pyridine ring annulation onto a thiophene scaffold—ranging from classical Friedländer and Gould–Jacobs reactions to modern metal-catalyzed, photo-induced, and electrochemical transformations; and (iii) multicomponent reactions for the simultaneous assembly of both heterocyclic rings. Furthermore, the strategic functionalization of preformed thienopyridine scaffolds to access complex tri- and polyheterocyclic systems is discussed. From a biological perspective, the review highlights the scaffold’s expanding therapeutic repertoire, including antibacterial, antifungal, and antiviral activities; potent anticancer applications targeting tumor-associated enzymes and emerging Proteolysis Targeting Chimera (PROTAC)/Deubiquitinase-Targeting Chimera (DUBTAC) technologies; and modulation of neurological, neuropsychiatric, and metabolic disorders. Finally, recent progress in the agrochemical utility of thienopyridines as insecticides and herbicide safeners is examined. Collectively, this work underscores the enduring relevance of the thienopyridine scaffold as a versatile platform for next-generation drug and agrochemical discovery.
SN - 1422-0067
ER -