Aim: In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A, lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages.
Results: Synthesized compounds effectively inhibited proinflammatory enzymes and cytokines.
Conclusion: A strong inhibition of secretory phospholipases A2 was exhibited by benzimidazole derivatives with trifluoromethyl and methoxy substitutions at position 4 of attached phenyl, whereas compound 8 containing pyridine ring substituted with amino group showed very potent 5-lipoxygenase inhibition. Molecular docking experiments were carried out to elucidate the molecular basis of the observed inhibitory activities.
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http://dx.doi.org/10.4155/fmc-2016-0062 | DOI Listing |
Mol Divers
January 2025
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, Guizhou, 550025, People's Republic of China.
This study focuses on the design, synthesis, and evaluation of benzimidazole derivatives for their anti-tumor activity against A549 and PC-3 cells. Initial screening using the MTT assay identified compound 5m as the most potent inhibitor of A549 cells with an IC of 7.19 μM, which was superior to the positive agents 5-Fluorouracil and Gefitinib.
View Article and Find Full Text PDFCrit Rev Oncog
January 2025
School of Pharmaceutical Sciences, Chhatrapati Shahu Ji Maharaj University, Kanpur 208024, India.
This article provides a basic summary of computational research on benzimidazole and its molecular targets in breast cancer (BC) drug discovery. The drug development process is streamlined, expenses are decreased, and the possibility of finding successful therapies for this difficult illness is increased with the use of computational tools. The utilization of benzimidazole derivatives in medication research and discovery is discussed, along with the results of benzimidazole derivative-related clinical trials conducted against blood cancer during the previous five years.
View Article and Find Full Text PDFRSC Adv
January 2025
Medicinal Chemistry Department, Faculty of Pharmacy, Minia University 61519 Minia Egypt.
Cancer is one of the leading causes of morbidity and mortality worldwide. One of the primary causes of cancer development and progression is epigenetic dysregulation, which is a heritable modification that alters gene expression without changing the DNA sequence. Therefore, targeting these epigenetic changes has emerged as a promising therapeutic strategy.
View Article and Find Full Text PDFCurr Top Med Chem
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Despite ongoing advancements in drug design and developments, breast cancer remains a serious and devastating disease and is ranked as the second most common illness in women. Breast cancer rates have increased significantly during the last 40 years. This necessitates the development of novel treatment techniques.
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