Generic placeholder image

Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

General Review Article

Fused and Substituted Pyrimidine Derivatives as Profound Anti-Cancer Agents

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

Volume 21 , Issue 7 , 2021

Published on: 21 July, 2020

Page: [861 - 893] Pages: 33

DOI: 10.2174/1871520620666200721104431

Price: $65


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.

Graphical Abstract

Rights & Permissions Print Export Cite as
© 2022 Bentham Science Publishers | Privacy Policy