2-Arylthio-5-iodo pyrimidine derivatives as non-nucleoside HBV polymerase inhibitors

Wang, Jie; Zhang, Liang; Zhao, Jianxiong; Zhang, Yu; Liu, Qingchuan; Tian, Chao; Liu, Junyi; Wang, Xiaowei

doi:10.1016/j.bmc.2018.02.003

Cited by 5 publications

(1 citation statement)

References 24 publications

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“…Pyrimidine is a heteroaryl system that consists of nitrogen at the first and third positions. In recent years, pyrimidine has gained focus for its use in many diseases as they have been used as antiviral ( Rashad and Ali, 2006 ; Rashad et al, 2009 ; Perlíková and Hocek, 2017 ; Wang et al, 2018 ), anticancer ( Galmarini et al, 2003 ; Song et al, 2011 ; Perlíková and Hocek, 2017 ), anti-hypertensive ( El-Hamouly et al, 2006 ; Ismail et al, 2006 ), anti-mycobacterial ( Garg et al, 2016 ; Khandazhinskaya et al, 2018 ), anti-microbial ( Okasha et al, 2016 ; Beyzaei et al, 2017 ; Marepu et al, 2018 ), anti-diabetic ( Spasov et al, 2017 ; Fang et al, 2018 ) and anti-inflammatory activities ( Zhang et al, 2017 ; Abdelgawad et al, 2018 ) .…”

Section: Introductionmentioning

confidence: 99%

A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure–Activity Relationship

et al. 2022

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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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Section: Introductionmentioning

confidence: 99%

A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure–Activity Relationship

et al. 2022

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Synthesis and Antiviral Efficacy of Pyrimidine Analogs Targeting Viral Pathways

Basha¹,

Chandana²

2023

ChemistrySelect

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To date, viruses are known to cause chronic to acute pathogenesis. Nevertheless, antiviral drugs have been known for their medicinal applications for the last few decades to treat infections caused by these pathogens. Despite advancements in the field of vaccination and antiviral drugs, there is a need for a molecule that can eradicate or control viral infection without getting resistance from pathogens will be a real challenge. This review covers possible ways to treat viral infections with pyrimidine and its mimics compared to known antiviral drugs. A comprehensive study of the report accomplished synthetic routes of pyrimidine analogs and their target‐specific antiviral potential. The present review article covers literature from 2018 to 2022.

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Pharmacological Potential of Pyrmidine Derivatives: A Review With Emphasis on Antiviral Effects and Virtual Screening Against Sars‐Cov‐2 Molecular Targets

et al. 2023

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The importance of R&D of new antivirals has been highly evident with the emergence of the pandemic caused by SARS‐CoV‐2. Pyrimidines are heterocyclic compounds with a broad biological spectrum. In this review we emphasize the antiviral application of pyrimidines. Scientific articles, drug and patent registrations were searched using terms involving antiviral pyrimidines. Between 2012 and 2022, more than 100 articles, which show the broad antiviral spectrum of these compounds, were added in this review. The publications of the last five years were prioritized. Anti‐HIV applications were found, their use more evident within the framework of antivirals; among others found were anti‐influenza, anti‐arboviral, and anti‐hepatitis viruses. The results found in the drug and patent databases corroborate the scenario observed in the analysis of scientific articles and demonstrate the importance of researching pyrimidine compounds in periods of great impact on global health. Additionally, through virtual screening of 119 pyrimidines from an in‐house library, we found seventeen pyrimidines with high binding potential with the Mpro and RdRp proteins of SARS‐CoV‐2. Almost all seventeen compounds showed good pharmacokinetic and toxicological profile, mainly compounds 150 and 151 being considered promising for biological evaluation against SARS‐CoV‐2.

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2-Arylthio-5-iodo pyrimidine derivatives as non-nucleoside HBV polymerase inhibitors

Cited by 5 publications

References 24 publications

A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure–Activity Relationship

A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure–Activity Relationship

Synthesis and Antiviral Efficacy of Pyrimidine Analogs Targeting Viral Pathways

Pharmacological Potential of Pyrmidine Derivatives: A Review With Emphasis on Antiviral Effects and Virtual Screening Against Sars‐Cov‐2 Molecular Targets

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