Fused and Substituted Pyrimidine Derivatives as Profound Anti-Cancer Agents

Author(s): Nahid Abbas*, Gurubasavaraja S.P. Matada, Prasad S. Dhiwar, Shilpa Patel, Giles Devasahayam

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 21 , Issue 7 , 2021

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Graphical Abstract:


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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Article Details

Year: 2021
Published on: 20 July, 2020
Page: [861 - 893]
Pages: 33
DOI: 10.2174/1871520620666200721104431
Price: $65

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