Discovery of novel thioquinazoline-N-aryl-acetamide/N-arylacetohydrazide hybrids as anti-SARS-CoV-2 agents: Synthesis, in vitro biological evaluation, and molecular docking studies

Abdel‐Mohsen, Heba T.; Omar, Mohamed A.; Kutkat, Omnia; Kerdawy, Ahmed M. El; Osman, Alaa A.; Gaballah, Mohamed S.; Mostafa, Ahmed; Ali, Mohamed A.; Diwani, Hoda I. El

doi:10.1016/j.molstruc.2022.134690

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Biological Efficacy Of Peptide Based Compounds Synthesized S...1

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Cited by 7 publications

(1 citation statement)

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“…In another recent report, the antiviral activity of two novel series of (tetrahydro)thioquinazoline- N -arylacetamides and (tetrahydro)thioquinazoline- N -arylacetohydrazides against SARS-CoV-2 was designed, synthesised, and studied by Mohsen and co-workers. 71 The thioquinazoline- N -arylacetamide (XXX) showed better efficacy among all with an antiviral activity (IC 50 ) of 21.4 μM ( Fig. 4 ).…”

Section: Biological Efficacy Of Peptide Based Compounds Synthesized S...mentioning

confidence: 99%

Recent updates on the biological efficacy of approved drugs and potent synthetic compounds against SARS-CoV-2

2023

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Section: Biological Efficacy Of Peptide Based Compounds Synthesized S...mentioning

confidence: 99%

Recent updates on the biological efficacy of approved drugs and potent synthetic compounds against SARS-CoV-2

2023

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Quinazoline‐oxindole hybrids as angiokinase inhibitors and anticancer agents: Design, synthesis, biological evaluation, and molecular docking studies

Syam,

Abd El‐Karim,

Abdel‐Mohsen

2024

Archiv der Pharmazie

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Two new sets of quinazoline‐oxindole 8a–l and quinazoline‐dioxoisoindoline 10a–d hybrids were designed as type II angiokinase inhibitors and anticancer agents. The design strategy was adjusted to account for the quinazoline scaffold's placement in the target kinases' hinge region, where it would form hydrogen bonding and hydrophobic interactions with the important amino acids to stabilize it, and the amide group's occupation in the gate region, which would direct the oxindole scaffold toward the hydrophobic back pocket. The two sets of quinazolines 8a–l and 10a–d displayed pronounced inhibitory activity on VEGFR‐2 (IC50 = 0.46–2.20 µM). The quinazoline‐oxindole hybrids 8d, 8f, and 8h displayed IC50 = 0.46, 0.49, and 0.49 µM, respectively. Compound 8f demonstrated potent multikinase activity with IC50 values of 0.95 and 0.67 µM against FGFR‐1 and BRAF, respectively. Additionally, compound 8f showed significant anticancer activity against National Cancer Institute's cancer cell lines, with GI50 reaching 1.21 µM. Analysis of the impact of compound 8f on the MDA‐MB‐231 cell line's cell cycle and apoptosis revealed that 8f stalled the cell cycle at the G2/M phase and promoted its necrosis.

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Synthesis, in silico and in vitro studies of novel quinazolinone derivatives as potential SARS-CoV-2 3CLpro inhibitors

Alamri,

Afzal,

Akhtar

et al. 2024

Arabian Journal of Chemistry

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Discovery of novel thioquinazoline-N-aryl-acetamide/N-arylacetohydrazide hybrids as anti-SARS-CoV-2 agents: Synthesis, in vitro biological evaluation, and molecular docking studies

Cited by 7 publications

References 46 publications

Recent updates on the biological efficacy of approved drugs and potent synthetic compounds against SARS-CoV-2

Recent updates on the biological efficacy of approved drugs and potent synthetic compounds against SARS-CoV-2

Quinazoline‐oxindole hybrids as angiokinase inhibitors and anticancer agents: Design, synthesis, biological evaluation, and molecular docking studies

Synthesis, in silico and in vitro studies of novel quinazolinone derivatives as potential SARS-CoV-2 3CLpro inhibitors

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