ReviewFrontiers in chemistry2022
A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure-Activity Relationship.
Review in Frontiers in chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 41 citations in OpenAlex.
- Dual Targeting Strategies in Cancer: Carbonic Anhydrase IX Inhibitors Targeting EGFR or VEGFR-2.Molecules (Basel, Switzerland) · 2026Review
- A Review on Anticancer Potential and Structure-Activity Relationships (SAR) of Novel EGFR/HER2 Inhibitors.Current topics in medicinal chemistry · 2026Review
- Novel Pyrrolopyrimidines as Inhibitors of CLK4 and HER2: Targeting Promising Anticancer Pathways.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2026Article
- Innovative Amino-Functionalization of Pyrido[2,3-Pharmaceuticals (Basel, Switzerland) · 2025Article
- Advances in Small-molecule Dual Inhibitors Targeting EGFR and HER2 Receptors as Anti-cancer Agents.Current medicinal chemistry · 2025Review
- Synthesis of Ethyl Pyrimidine-Quinolincarboxylates Selected from Virtual Screening as Enhanced Lactate Dehydrogenase (LDH) Inhibitors.International journal of molecular sciences · 2024Article
- Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFRRSC advances · 2024Article
- Article
- Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry · 2023Article
- Potent PROTACs Targeting EGFR Mutants in Drug Discovery.ACS medicinal chemistry letters · 2022Article
- Targeting the EGFR signaling pathway in cancer therapy: What's new in 2023?Expert opinion on therapeutic targetsReview
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Epidermal growth factor receptor (EGFR) belongs to the family of tyrosine kinase that is activated when a specific ligand binds to it. The EGFR plays a vital role in the cellular proliferation process, differentiation, and apoptosis. In the case of cancer, EGFR undergoes uncontrolled auto-phosphorylation that results in increased cellular proliferation and decreased apoptosis, causing cancer promotion. From the literature, it shows that pyrimidine is one of the most commonly studied heterocycles for its antiproliferative activity against EGFR inhibition. The authors have collated some interesting results in the heterocycle-fused pyrimidines that have been studied using different cell lines (sensitive and mutational) and in animal models to determine their activity and potency. It is quite clear that the fused systems are highly effective in inhibiting EGFR activity in cancer cells. Therefore, the structure-activity relationship (SAR) comes into play in determining the nature of the heterocycle and the substituents that are responsible for the increased activity and toxicity. Understanding the SAR of heterocycle-fused pyrimidines will help in getting a better overview of the molecules concerning their activity and potency profile as future EGFR inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.