Thienopyrimidine Derivatives in Medicinal Chemistry

Thienopyrimidines constitute a class of fused heterocyclic scaffolds formed by the fusion of a thiophene ring with a pyrimidine nucleus. Their structural analogy to purine bases has inspired extensive exploration of three principal isomeric frameworks—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—in drug discovery. Owing to their planar aromatic systems and capacity for diverse substitution patterns, thienopyrimidine derivatives have emerged as versatile pharmacophores with demonstrated activities across oncology, anti-infective and anti-inflammatory fields. Synthetic accessibility via multicomponent reactions and cyclization strategies has facilitated rapid generation of libraries, while fragment-based optimisation has yielded potent kinase inhibitors targeting receptors such as FLT3, FGFR-1 and EGFR. In parallel, modifications at key positions have produced agents acting on enzymes like dihydrofolate reductase and squalene epoxidase, underscoring the global significance of thienopyrimidine scaffolds in addressing antimicrobial resistance and chemotherapeutic challenges.

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Thienopyrimidine Derivatives in Medicinal Chemistry publication trend

The graph below shows the total number of articles in thienopyrimidine derivatives in medicinal chemistry across all publications each year (not limited to Nature Index journals).

Technical terms

Thienopyrimidine: A heterocyclic scaffold combining a thiophene ring with a pyrimidine moiety, often used as a drug-discovery core.

Molecular docking: A computational technique that predicts the preferred orientation of a small molecule when bound to a protein target.

Kinase inhibitor: A compound that interferes with the enzymatic activity of protein kinases, thereby modulating cell signalling pathways.

Apoptosis: A programmed cell-death process characterised by cell shrinkage, DNA fragmentation and membrane blebbing.

Minimum inhibitory concentration (MIC): The lowest concentration of an antimicrobial agent required to prevent visible growth of a microorganism.

References

1. In Silico Screening and Anticancer-Apoptotic Evaluation of Newly Synthesized Thienopyrimidine/Sulfonamide Hybrids. International Journal of Molecular Sciences (2023).
2. Antimicrobial Evaluation of Sulfonamides after Coupling with Thienopyrimidine Coplanar Structure. Pharmaceuticals (2024).
3. Designing Potent Anti-Cancer Agents: Synthesis and Molecular Docking Studies of Thieno[2,3-d][1,2,4]triazolo[1,5-a]pyrimidine Derivatives. Molecules (2024).