The rationale behind drug design is the strategic utilization of heterocyclic fragments with specific
physicochemical properties to form molecular targeted agents. Among the heterocyclic molecules, pyrimidine
has proved to be a privileged pharmacophore for various biological cancer targets. The anti-cancer potential of
small molecules with fused and substituted pyrimidines can be enhanced through bioisosteric replacements and
altering their ADME parameters. Although several small molecules are used in cancer chemotherapy, oncology
therapeutics has various limitations, especially in their routes of administration and their concurrent side effects.
Such pernicious effects may be overcome, via selective biological targeting. In this review, the biological targets,
to inhibit cancer, have been discussed. The structural activity relationship of fused and substituted
pyrimidines was studied. Eco-friendly synthetic approaches for pyrimidine derivatives have also been discussed.
This review will give an insight to scientists and researchers of medicinal chemistry discipline to design small
molecules having a pyrimidine scaffold with high anti-cancer potential.
Keywords: Apoptosis, anti-proliferative, structural activity relationship, pyrimidine, green chemistry, synthesis, SAR.
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