Pyridopyrimidine is an important heterocyclic scaffold widely explored in anticancer drug discovery. Its structural similarity to purine enables effective interaction with various biological targets, mainly kinases involved in cancer progression. This manuscript presents recent developments reported between 2021 and 2026, focusing on the biological evaluation, and structure–activity relationships of pyridopyrimidine derivatives. Many of these synthesized compounds act as inhibitors of key targets such as EGFR, CDK4/6, and the PI3K/mTOR pathway, which are closely associated with tumor growth, survival, and resistance mechanisms. Other targets such as ATR and PIM are also explored. Recent studies show that structural modifications, including substitution on the core ring and hybridization with pharmacologically active moieties like triazoles and thiazolidinediones, significantly improve anticancer activity. Several derivatives have demonstrated strong antiproliferative effects against different cancer cell lines and are capable of inducing apoptosis and cell cycle arrest. In addition, molecular docking and other computational studies support their binding efficiency and help explain their mechanisms of action. There is also increasing interest in the development of dual-target or multi-target inhibitors to overcome drug resistance and enhance therapeutic effectiveness. Overall, pyridopyrimidine- and pyridopyrimidinones-based compounds continue to show great promise as potential anticancer agents. Further research combining synthetic chemistry, biological studies, and computational approaches may lead to the development of more effective and safer drugs in the future.
OBJECTIVES
Epilepsy is a chronic neurological disorder affecting nearly 50 million people worldwide and is characterized by recurrent seizures caused by abnormal neuronal activity. Conventional therapies, including antiepileptic drugs, growth factors, and gene therapy, are often limited by poor blood-brain barrier (BBB) penetration, drug resistance, adverse effects, and low bioavailability. This review summarizes recent advances in nanocarrier-based drug delivery systems for improving epilepsy treatment.
METHODS
A comprehensive review of peer-reviewed articles, patents, and clinical studies was conducted to evaluate lipid-based, vesicular, polymeric, dendrimer, and inorganic nanocarriers. Their formulation strategies, BBB transport mechanisms, therapeutic applications, clinical progress, and future prospects were critically analysed.
KEY FINDINGS
Nanocarriers enhance the solubility, stability, bioavailability, controlled release, and brain targeting of antiepileptic drugs. Liposomes, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanoparticles, dendrimers, nanoemulsions, and metallic nanoparticles have demonstrated improved BBB penetration, prolonged drug action, reduced toxicity, and enhanced seizure control in preclinical studies. Despite promising outcomes, challenges related to large-scale manufacturing, long-term safety, regulatory approval, and clinical translation remain.
CONCLUSIONS
Nanomedicine represents a promising approach for overcoming the limitations of conventional epilepsy therapy by enabling efficient brain-targeted drug delivery. Further optimization, safety evaluation, and clinical validation are essential to support the successful translation of nanocarrier-based therapies into clinical practice.
Abhishek Chauhan, Ankush Kumar, Ankit Awasthi et al.· The Journal of pharmacy and...· 0 citations