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...

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...

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...

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...

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...

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...

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...

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...

Introduction: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are used in treating pathologic conditions such as fever, pain and inflammation by inhibiting cyclooxygenase and consequently prostaglandin production. Recently , the discovery of different isoforms of this enzyme, Cyclooxygenase-1 (COX-1) andCyclooxygense-2 (COX-2), has led to the synthesis and introduction of novel drugs with select...