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.