Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19

Qureshi, Faiza; Nawaz, Muhammad; Hisaindee, Soleiman; Almofty, Sarah Ameen; Ansari, Mohammad Azam; Jamal, Qazi Mohammad Sajid; Ullah, Nisar; Taha, Muhammad; Alshehri, Ohood; Huwaimel, Bader; Break, Mohammed Khaled Bin

doi:10.1016/j.arabjc.2022.104366

Cited by 8 publications

(9 citation statements)

References 59 publications

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“…The 30,000 cells/well were seeded in 96-well plates containing DMEM, fetal bovine serum, L-glutamine, penicillin, streptomycin and selenium chloride and were kept in a CO 2 incubator (Thermo-Fisher Scientific, Waltham, MA, USA) at 37 °C. The cells were then treated with varying concentration of Ag-C-1 and Ag-C-3 and further incubated for 48 h [ 35 ]. In the control group, NPs were not added.…”

Section: Methodsmentioning

confidence: 99%

Hydrothermal Synthesis of Multifunctional Bimetallic Ag-CuO Nanohybrids and Their Antimicrobial, Antibiofilm and Antiproliferative Potential

2022

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The rapidly growing global problem of infectious pathogens acquiring resistance to conventional antibiotics is an instigating reason for researchers to continue the search for functional as well as broad-spectrum antimicrobials. Hence, we aimed in this study to synthesis silver–copper oxide (Ag-CuO) nanohybrids as a function of Ag concentration (0.05, 0.1, 0.3 and 0.5 g) via the one-step hydrothermal method. The bimetallic Ag-CuO nanohybrids Ag-C-1, Ag-C-2, Ag-C-3 and Ag-C-4 were characterized for their physico-chemical properties. The SEM results showed pleomorphic Ag-CuO crystals; however, the majority of the particles were found in spherical shape. TEM results showed that the Ag-CuO nanohybrids in formulations Ag-C-1 and Ag-C-3 were in the size range of 20–35 nm. Strong signals of Ag, Cu and O in the EDX spectra revealed that the as-synthesized nanostructures are bimetallic Ag-CuO nanohybrids. The obtained Ag-C-1, Ag-C-2, Ag-C-3 and Ag-C-4 nanohybrids have shown their MICs and MBCs against E. coli and C. albicans in the range of 4–12 mg/mL and 2–24 mg/mL, respectively. Furthermore, dose-dependent toxicity and apoptosis process stimulation in the cultured human colon cancer HCT-116 cells have proven the Ag-CuO nanohybrids as promising antiproliferative agents against mammalian cancer.

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Section: Methodsmentioning

confidence: 99%

Hydrothermal Synthesis of Multifunctional Bimetallic Ag-CuO Nanohybrids and Their Antimicrobial, Antibiofilm and Antiproliferative Potential

2022

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“…Therefore, using MW irradiation for rapid reaction, and synthesis. The comparison of MW with conventional methods and the advantages of MW in synthetic heterocyclic chemistry [27,28] . On the other hand, the benefits of this procedure are as follows: (a) Promoting the chemical reaction by reducing the reaction time from hours to minutes and second.…”

Section: Introductionmentioning

confidence: 99%

“…Recent applications of MW have emerged as a powerful technique for the preparation of heterocyclic compounds and thus, it has been wiedly used spread in various areas of organic reactions, such as ring formation by cyclization, cyclocondensation, cycloaddition, and nucleophilic substitution reactions, have been reported. [27,28] Therefore, using MW irradiation for rapid reaction, and synthesis. The comparison of MW with conventional methods and the advantages of MW in synthetic heterocyclic chemistry.…”

Section: Introductionmentioning

confidence: 99%

“…The comparison of MW with conventional methods and the advantages of MW in synthetic heterocyclic chemistry. [27,28] On the other hand, the benefits of this procedure are as follows: (a) Promoting the chemical reaction by reducing the reaction time from hours to minutes and second. (b) Reduction of environmental pollution as reactions can occur solvent-free to offer low cost together with a green process.…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, using microwave (MW) in the synthesis of heterocyclic compounds has been prevalent for almost 20 years, mainly because of the convenience of temperature control, as it is far faster and better in results than conventional techniques. Recent applications of MW have emerged as a powerful technique for the preparation of heterocyclic compounds and thus, it has been wiedly used spread in various areas of organic reactions, such as ring formation by cyclization, cyclocondensation, cycloaddition, and nucleophilic substitution reactions, have been reported [27,28] . Therefore, using MW irradiation for rapid reaction, and synthesis.…”

Section: Introductionmentioning

confidence: 99%

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Microwave‐Assisted Synthesis of Phthalazinone Derivatives with Biological Activity and In Silico Antiproliferative Studies

Abubshait

Almalih

et al. 2022

ChemistrySelect

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Several nitrogen heterocycles are considered as privileged scaffolds in drug discovery and are present in several drugs with diverse biological activities. Herein, we report the synthesis and characterization of phthalazinone derivatives by using a green synthesis protocol under microwave irradiation. The reduced reaction time and high yield are some of the advantages that render this procedure a greener alternative to conventional chemical synthesis. The structures of all new derivatives were confirmed by spectral analysis. Synthesized derivatives show an effective antimicrobial effect. These compounds were also screened for their in vitro anticancer activity against colon cancer cell line (HCT116). Among the synthesized derivatives are exhibited the highest anticancer activity with IC50 of 28.97±0.11, 66.25±0.14 and 76.04±0.09 μM respectively. The antiproliferative activity was supported by molecular docking studies that showed that phthalazinone derivatives would potentially act through inhibition of PARP. The simulation studies substantiated the biological results as an active compounds in term of binding interactions and scores.

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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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Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19

Cited by 8 publications

References 59 publications

Hydrothermal Synthesis of Multifunctional Bimetallic Ag-CuO Nanohybrids and Their Antimicrobial, Antibiofilm and Antiproliferative Potential

Hydrothermal Synthesis of Multifunctional Bimetallic Ag-CuO Nanohybrids and Their Antimicrobial, Antibiofilm and Antiproliferative Potential

Microwave‐Assisted Synthesis of Phthalazinone Derivatives with Biological Activity and In Silico Antiproliferative Studies

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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