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Updated: Mar 14, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Roles of Pyridine and Pyrimidine Derivatives as Privileged Scaffolds in Anticancer Agents
Supaluk Prachayasittikul1, Ratchanok Pingaew2, Apilak Worachartcheewan1
1Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand.
Background:
Cancer has been considered to be a global health concern due to the impact of disease on the quality of life. The continual increase of cancer cases as well as the resistance of cancer cells to the existing drugs have driven the search for novel anticancer drugs with better potency and selectivity, improved pharmacokinetic profiles, and minimum toxicities. Pyridine and pyrimidine are presented in natural products and genetic materials. These pyridine/pyrimidine core structures have been noted for their roles in many biological processes as well as in cancer pathogenesis, which make such compounds become attractive scaffolds for discovery of novel drugs.
Results & Conclusion:
In the recent years, pyridine- and pyrimidine-based anticancer drugs have been developed based on structural modification of these core structures (i.e., substitution with moieties and rings, conjugation with other compounds, and coordination with metal ions). Detailed discussion is provided in this review to highlight the potential of these small molecules as privileged scaffolds with attractive properties and biological activities for the search of novel anticancer agents.
Insights
Pyridine and pyrimidine compounds are promising scaffolds for developing new anticancer drugs. Structural modifications enhance their potency, selectivity, and pharmacokinetic profiles for improved cancer treatment.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Cancer poses a significant global health challenge, necessitating novel therapeutic agents.
- Existing cancer treatments face limitations due to drug resistance and toxicity.
- Pyridine and pyrimidine structures are integral to biological processes and cancer development, making them attractive drug discovery scaffolds.
Purpose of the Study:
- To review the potential of pyridine and pyrimidine derivatives as anticancer agents.
- To highlight structural modifications leading to enhanced drug properties.
- To underscore the significance of these scaffolds in novel drug development.
Main Methods:
- Literature review of pyridine and pyrimidine-based anticancer compounds.
- Analysis of structural modifications and their impact on biological activity.
- Discussion of pharmacokinetic profiles and toxicity considerations.
Main Results:
- Recent advancements include structural modifications like substitution, conjugation, and metal coordination.
- Pyridine and pyrimidine scaffolds demonstrate significant potential for developing potent and selective anticancer drugs.
- These modifications aim to improve efficacy and reduce adverse effects.
Conclusions:
- Pyridine and pyrimidine derivatives represent privileged scaffolds for anticancer drug discovery.
- Their versatile structures allow for optimization of potency, selectivity, and pharmacokinetic properties.
- Continued research into these compounds promises novel therapeutic strategies for cancer treatment.
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