Rhodanine Derivatives Containing 5‐Aryloxypyrazole Moiety as Anti‐inflammatory and Anticancer Agents

Zhu, Lin; Ye, Chao; Chen, Shuang; Fang, Yuqi; Zhang, Yu; Zhang, Tianyi

doi:10.1002/cbdv.202301844

Chemistry & Biodiversity

2024

DOI: 10.1002/cbdv.202301844

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Rhodanine Derivatives Containing 5‐Aryloxypyrazole Moiety as Anti‐inflammatory and Anticancer Agents

Lin Zhu,

Chao Ye,

Shuang Chen

et al.

Abstract: In this study, a series of rhodanine derivatives containing 5‐aryloxypyrazole moiety were identified as potential agents with anti‐inflammatory and anticancer properties. Most of the synthesized compounds demonstrated anti‐inflammatory and anticancer activity.

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2024

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Cited by 3 publications

References 26 publications

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Synthesis and Biological Evaluation of Isoaurone Derivatives as Anti‐inflammatory Agents

Bai,

Ye,

Liu

et al. 2024

Chemistry & Biodiversity

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Twenty‐eight isoaurone derivatives with 1,2,4‐triazole moieties were synthesized using a fragment‐based design strategy, and their anti‐inflammatory activity was investigated. The anti‐inflammatory effect of the most active derivatives, 14e (41.82%), was dose‐dependent and higher than the values for celecoxib (31.82%). Compound 14e was almost non‐toxic and inhibited different concentrations of nitric oxide (NO). The western blotting results demonstrated that cyclooxygenase‐2 (COX‐2) expression was elevated when the macrophages were exclusively treated with LPS. However, compound 14e effectively suppressed the LPS‐induced COX‐2 upregulation. Subsequent investigation revealed that 14e is a promising compound capable of inhibiting the downstream signaling of COX‐2. With the above interesting biological profile, molecular 14e could be a promising lead to develop novel anti‐inflammatory agents.

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Synthesis and Biological Evaluation of Isoaurone Derivatives as Anti‐inflammatory Agents

Bai,

Ye,

Liu

et al. 2024

Chemistry & Biodiversity

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Ultrasound Irradiated Synthesis and Characterization of Dispiropyrrolidines Grafted Rhodanine‐3‐acetic Acid Moiety: Anticancer and In Silico Activities

Sundaram,

Kannapiran,

Ravi

et al. 2024

ChemistrySelect

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Fourteen dispiropyrrolidines were synthesized through a [3 + 2] cycloaddition reaction using ultrasound irradiation involving isatin, sarcosine, and derivatives of 5‐benzylidine rhodanine‐3‐acetic acid and characterized using UV–visible, IR, and NMR analysis. The inhibitory potential of these compounds against the HeLa cell line was assessed using the MTT assay. Compounds 4i and 4j displayed promising activity, showing IC50 values of 71.41 µM and 70.54 µM, respectively. The exhibited inhibitory effects compared to Sorafenib, a reference drug with an IC50 of 10.78 µM. In pursuit of a better understanding of molecular interactions, a molecular docking study was performed employing AutoDock Vina, focusing on the HPV protein. Among the synthesized compounds, the most potent molecules 4i and 4j showed a binding affinity of −7.4 and −7.3 Kcal/mol, respectively.

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Novel isatin conjugates endowed with analgesic and anti-inflammatory properties: design, synthesis and biological evaluation

Brown,

Girgis,

Patel

et al. 2024

Future Medicinal Chemistry

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Rhodanine Derivatives Containing 5‐Aryloxypyrazole Moiety as Anti‐inflammatory and Anticancer Agents

Abstract: In this study, a series of rhodanine derivatives containing 5‐aryloxypyrazole moiety were identified as potential agents with anti‐inflammatory and anticancer properties. Most of the synthesized compounds demonstrated anti‐inflammatory and anticancer activity.

Cited by 3 publications

References 26 publications

Synthesis and Biological Evaluation of Isoaurone Derivatives as Anti‐inflammatory Agents

Synthesis and Biological Evaluation of Isoaurone Derivatives as Anti‐inflammatory Agents

Ultrasound Irradiated Synthesis and Characterization of Dispiropyrrolidines Grafted Rhodanine‐3‐acetic Acid Moiety: Anticancer and In Silico Activities

Novel isatin conjugates endowed with analgesic and anti-inflammatory properties: design, synthesis and biological evaluation

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