نتایج جستجو برای: cox 2 inhibitory
تعداد نتایج: 2641865 فیلتر نتایج به سال:
Swertia alata C.B Clarke (Gentianaceae) is a well-reported plant in the traditional system of medicine. The present study was intended to isolate phytoconstituents from ethanolic extract aerial parts S. alata; and evaluate for vitro COX-1/COX-2 inhibition activity, vivo anti-inflammatory ulcerogenic activity. Phytoisolation involved partitioning into petroleum ether chloroform soluble fractions...
سرطان سومین عامل مرگ در ایران است و سالانه حدود 30 هزار نفر در ایران بر اثر ابتلا به انواع سرطان جان خود را از دست می دهند. سرطان مری یا esophagus cancer در بین سرطان ها رتبه ششم از نظر شیوع و از نظر مرگ و میر در رتبه نهم سرطان ها دارد. هدف از این مطالعه ارزیابی بررسی بیان ژن پروستاگلاندین اندوپروکسید سنتتاز 2 (cox-2) در سرطان مری می باشد. cox ها (cyclo-oxygenases)، cox-1و cox-2، آنزیم های نظار...
Abstract The selective inhibition of enzymes that catalyze the conversion arachidonic acid to inflammatory eicosanoids represents a promising approach for cancer therapy. This study, therefore, focuses on incorporation metabolically stable, sterically demanding, and hydrophobic carboranes into existing dual cycloxygenase‐2 (COX‐2)/5‐lipoxygenase (5‐LO) inhibitors are key in biosynthesis eicosan...
PURPOSE Cyclooxygenase (COX) is the main pharmacodynamic target of nonsteroidal anti-inflammatory drugs (NSAIDs). We investigated the inhibitory effects on COX-2 after NSAIDs administration using a lipopolysaccharide (LPS)-derived COX-2 induction model in whole blood, according to the genotypes of COX-2 single-nucleotide polymorphisms (SNPs). PATIENTS AND METHODS Seven genotypes of COX-2 SNPs...
A series of NO-donor diarylimidazoles derived from the lead compound Cimicoxib were synthesized and evaluated for their COX-2 inhibitory activity and their stability in whole blood as well as for vasodilator properties. The products are partly transformed into the corresponding alcohols following 24-h incubation in whole blood. All of them display good COX-1/COX-2 selectivity, but are less pote...
In order to develop new selective COX-2 inhibitors, a new series of 2-phenyl-4H-chromen-4-one derivatives possessing a methylsulfonyl pharmacophore group at the para position of the C-4 phenyl ring were designed, synthesized, and evaluated for cyclooxygenase-2 inhibitory activity. In vitro COX-1/COX-2 isozyme inhibition structure-activity studies identified 3-(benzyloxy)-2-[4-(methylsulfonyl)ph...
Epidermal growth factor receptor (EGFR) activation is a major cause of metastasis in many cancers, such as head and neck squamous cell carcinoma (HNSCC). However, whether the induction of cyclooxygenase-2 (COX-2) mediates EGF-enhanced HNSCC metastasis remains unclear. Interestingly, we found that EGF induced COX-2 expression mainly in HNSCC. The tumor cell transformation induced by EGF was repr...
A new briarane-type diterpenoid, named 2-acetoxyverecynarmin C, was isolated from the methanolic extract of an octocoral, Pennatula aculeata, that exhibited cyclooxygenase (COX) inhibitory activity. The structure of the compound was elucidated by ESI-HRMS, 1D and 2D NMR spectroscopy and comparison of the measured spectral data with those reported in the literature. The relative stereochemistry ...
a group of 1,3-biarylhydrazide derivatives possessing a cox-2 azido pharmacophore at the para- position of the c-1 phenyl ring in conjunction with a n-3 phenyl or substituted-phenyl ring (4-f,4-cl,4-ome) were designed and synthesized based on nucleophilic substitution reaction. a molecular modelling study of these compounds showed that the designed molecules were well bound with the active site...
NS-398 [N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide], a selective inhibitor of cyclooxygenase-2 (COX-2), inhibited proliferation induced by platelet-derived growth factor (PDGF) in Swiss 3T3 fibroblasts. The effect of NS-398 was found to be concentration-dependent. The half-maximal effect occurred at approximately 0.1 microM. NS-398 decreased mitogenesis at subsaturating PDGF concentrat...
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