Design, synthesis, and cytotoxicity of ibuprofen-appended benzoxazole analogues against human breast adenocarcinoma

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(4), P. 1283 - 1294

Published: Jan. 1, 2024

A library of novel ibuprofen-appended benzoxazole analogues (7a-l) was synthesized

Language: Английский

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Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Antibiotics, Journal Year: 2023, Volume and Issue: 12(7), P. 1220 - 1220

Published: July 22, 2023

Bacterial infections have attracted the attention of researchers in recent decades, especially due to special problems they faced, such as their increasing diversity and resistance antibiotic treatment. The emergence development SARS-CoV-2 infection stimulated even more research find new structures with antimicrobial antiviral properties. Among heterocyclic compounds remarkable therapeutic properties, benzimidazoles, triazoles stand out, possessing antimicrobial, antiviral, antitumor, anti-Alzheimer, anti-inflammatory, analgesic, antidiabetic, or anti-ulcer activities. In addition, literature last decade reports benzimidazole-triazole hybrids improved biological properties compared simple mono-heterocyclic compounds. This review aims provide an update on synthesis methods these hybrids, along activities, well structure-activity relationship reported literature. It was found that presence certain groups grafted onto benzimidazole and/or triazole nuclei (-F, -Cl, -Br, -CF3, -NO2, -CN, -CHO, -OH, OCH3, COOCH3), some heterocycles (pyridine, pyrimidine, thiazole, indole, isoxazole, thiadiazole, coumarin) increases activity hybrids. Also, oxygen sulfur atom bridge connecting rings generally mentions only benzimidazole-1,2,3-triazole Both for additional ring activity, which is agreement three-dimensional binding mode summarizes advances derivatives potential agents covering articles published from 2000 2023.

Language: Английский

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Design and synthesis of Meldrum's acid based 7-azaindole anchored 1,2,3-triazole hybrids as anticancer agents

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(5), P. 1709 - 1721

Published: Jan. 1, 2024

A series of Meldrum's acid, 7-azaindole and 1,2,3-triazole hybrids were synthesized evaluated for in vitro anticancer activity against five cancer cell lines viz. MCF-7 (breast cancer), HeLa (cervical DU-145 (prostate HepG2 (liver cancer) K562 (myelogenous leukemia cell).

Language: Английский

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Mixed ligand 4‑hydroxy acetanilide-febuxostat complexes of Co(II),- Ni(II), Cu(II) and Zr(IV): Synthesis, structural characterization, DFT calculations, antibacterial, antioxidant and molecular docking studies

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1308, P. 138115 - 138115

Published: March 21, 2024

Language: Английский

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Antioxidant activity of novel 4H- chromene tethered 1,2,3-Triazole Analogues: Synthesis and molecular docking studies

Results in Chemistry, Journal Year: 2023, Volume and Issue: 5, P. 100987 - 100987

Published: Jan. 1, 2023

Novel 4H chromene coupled triazole hybrids 8a-l were synthesized through a hassle free multicomponent one pot synthesis and click chemistry protocols. The structures of novel compounds established by interpretation 1H NMR, 13C IR Mass spectral data. screened for their invitro antioxidant activity employing DPPH Hydrogen peroxide radical scavenging assays, using Ascorbic acid as standard reference. 8h 8i exhibited superior quenching percentage with IC50 value 1.29 ± 0.35 1.23 0.34 µM respectively, compared to the (1.46 0.52 µM) acid. Compounds 8f, 8j 8k also demonstrated best 3.02 0.62, 2.45 0.53 3.18 0.25 in comparison molecular docking studies target against crystal structure NADPH oxidase endorsed scores binding interactions, are agreement experimental

Language: Английский

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Synthesis of New Chroman‐4‐one Based 1,2,3‐Triazole Analogues as Antioxidant and Anti‐Inflammatory Agents

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(7)

Published: May 8, 2024

Abstract A library of new chroman‐4‐one based 1,2,3‐triazole analogues were synthesized involving a series condensation, cyclization, Suzuki coupling and copper catalysed click chemistry protocols. The newly compounds 8a – l screened for their invitro antioxidant anti‐inflammatory activities by employing Ascorbic acid Diclofenac as reference drugs respectively. compound without any substituent on benzyl ring ( ), with ‐Cl in para position (8i) , ethoxy 8k) exhibited potent higher percentage inhibition. To understand binding affinities, molecular docking study these three performed against NADPH oxidase presented outstanding scores promising interactions like H‐bond hydrophobic.

Language: Английский

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An updated review on 1,2,3-/1,2,4-triazoles: synthesis and diverse range of biological potential

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: July 27, 2024

Language: Английский

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Synthesis of Novel Substituted 4-[1-(1-Phenyl-1H-[1,2,3]triazol-4-yl-methyl)-1H-benzimidazol-2-yl]piperidine-1-carboxylic Acids tert-Butyl Esters. Evaluation of Cytotoxic and Antimicrobial Activity

Russian Journal of General Chemistry, Journal Year: 2025, Volume and Issue: 95(3), P. 538 - 547

Published: March 1, 2025

Language: Английский

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pH‐Dependent Chromogenic and Smartphone‐Assisted Detection of Fe(III) by Acid‐Sensitive 1,2‐Biphenyl‐Substituted Benzimidazole 1,2,3‐Triazole Hybrids: In Vitro Anticancer Property Evaluation and In Silico Inhibition of Breast Cancer Estrogen Receptor Mutant L536S

Applied Organometallic Chemistry, Journal Year: 2025, Volume and Issue: 39(5)

Published: April 9, 2025

ABSTRACT The detection of Fe(III) ions and monitoring pH conditions are vital for safety, efficiency, sustainability in scientific research, environmental management, industrial applications. In this study, two 1,2‐biphenyl‐substituted benzimidazole‐1,2,3‐triazole hybrids, Pact Oact, were designed, developed, characterized by various spectroscopic techniques including single‐crystal XRD analysis. demonstrated high sensitivity selectivity towards under physiological pH, confirmed through visual tests, UV–visible, fluorescence spectroscopy, with limits (LOD) 0.3 (emission) 0.07 nM (absorption). A 1:1 ligand‐to‐metal binding ratio was established Job's plot supported NMR, mass, VSM, FT‐IR analyses. RGB tool (LOD: 3.4 mM) a paper kit test its portable reversible nature, validated EDTA suggesting potential molecular logic gate Environmental highlighted real water sample analysis, while DFT calculations identified favorable metal sites. Additionally, exhibited highly acidic conditions, containing nitro group, showed superior vitro anticancer activity against HeLa cells compared to Pact, higher score (−9.10 kcal/mol vs. −8.63 kcal/mol) docking studies the breast cancer estrogen receptor mutant L536S (PDB ID: 6sbo). Antioxidant assays further Oact's enhanced radical scavenging potential.

Language: Английский

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Design, Synthesis of Novel 1,2,3‐Triazole Pendent Quinazolinones and Their Cytotoxicity against MCF‐7 Cell Line

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(12)

Published: Sept. 14, 2023

A library of 6-(((1-(substitutedphenyl)-1H-1,2,3-triazol-4-yl)methyl) amino)-3-methylquinazolin-4(3H)-one analogues synthesized from Isatin precursor through a series nitration, reduction, hydrolysis, cyclization and click reaction. The structures compounds were characterized by spectral data including IR, 1 H-NMR, 13 C NMR Mass. novel quinazolinone - 1,2,3-triazoles screened for their cytotoxicity against the human breast adenocarcinoma cell lines MCF-7 MTT assay. 4-Isopropyl 2-bromo substituted executed high activity line with IC50 value 10.16±0.07 μM 11.23±0.20 compared to Doxorubicin whose is 10.81±0.03 μM. remaining good moderate. Further, molecular docking studies crystal structure Epidermal Growth Factor Receptor delivered best binding energies interactions such as H-bond hydrophobic are inevitable. predicted pharmacokinetic properties results showed that these have more drug likeness properties.

Language: Английский

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