A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

Cyclooxygenase-2 (COX-2) has a pivotal role in the pathogenesis of the lung cancer. It is known that COX-2 negatively regulates the activity of a number of tumor suppressors, including p53. Consequently, inhibition of COX-2 signaling is anticipated to be a promising approach to stabilize p53 functionality. In this regard, we investigated the effect of COX-2 signaling blockade on p53 and COX-2 e...

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

Design of selective cyclooxygenase-2 (COX-2) inhibitors is still a challenging task because of active site similarities between COX isoenzymes. To help with this issue, we tried to generate a 3D-QSAR (3 dimensional quantitative structure activity relationship) model that might reflect the essential features of COX-2 active sites. Compounds in a series of resveratrol derivatives inhibitors with ...

background: lymphomas are a group of malignancies affecting b, t and nk cells. cox-2 enzyme is one of the known inflammatory factors which increase in the inflammation process. increase in cox-2 expression inhibits apoptosis and increases tumor cells invasion and angiogenesis. increase in the cox-2 gene expression is seen in a group of cancers .specific cox-2 inhibition also can be beneficial i...

background : gastric cancer is the one of the most prevalent reason of cancer-related death in the world. survival of patients after surgery involves identifying risk factors. there are various models to detect the effect of risk factors on patients’ survival. the present study aims at evaluating these models. methods : data from 330 gastric cancer patients diagnosed at the iran cancer institut...

survival analysis is a set of methods used for analysis of the data which exist until the occurrence of an event. this study aimed to compare the results of the use of the semi-parametric cox model with parametric models to determine the factors influencing the length of stay of patients in the inpatient units of women hospital in tehran, iran. in this historical cohort study all 3421 charts of...

Despite the important role of both cyclooxygenase (COX) isoforms (i.e. COX-1 and COX-2) in maintenance of hypersensitivity following peripheral nerve injury, their role in the development of neuropathic pain is not clear. The present study was undertaken to determine the effect of COX inhibitors to address the potential role of COX isozymes in the development of neuropathic pain in rats after c...

A new group of 4-(Imidazolylmethyl) quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitro anti breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 value...