2010
DOI: 10.1016/j.bmc.2009.12.060
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Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors

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Cited by 51 publications
(36 citation statements)
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“…27-34 Consistent with this observation, the 2-furylquinoline-4-carbonyl substructure is present in 170 HTS library members available in the University of Minnesota and the NIH MLPCN screening libraries and in many of our own HTS hits (Figure 1). As a result of marked A3 inhibition in HTS screening, a low toxicity profile against human cells, and the lack of PAINS warnings, we initiated a structural optimization campaign to refine 1 for potency and selectivity.…”
Section: Introductionsupporting
confidence: 71%
“…27-34 Consistent with this observation, the 2-furylquinoline-4-carbonyl substructure is present in 170 HTS library members available in the University of Minnesota and the NIH MLPCN screening libraries and in many of our own HTS hits (Figure 1). As a result of marked A3 inhibition in HTS screening, a low toxicity profile against human cells, and the lack of PAINS warnings, we initiated a structural optimization campaign to refine 1 for potency and selectivity.…”
Section: Introductionsupporting
confidence: 71%
“…In contrast with the traditional NSAIDs which belong to different categories of chemical structures, selective COX-2 inhibitors can be classified into three groups ( Figure 1): (1) diaryl ethers with methanesulfonamide at position-2 of one ring, Nemisulide and CGP-28237 can be considered as lead compounds in this class 8 ; (2) trans-stilbenoids, such as resveratrol, a natural product found in grapes and other food products 9 ; (3) heterocyclic systems (such as 1,2,4 triazole 10,11 , imidazole 12 , pyrazol 13 , quinoline 14 , indol 15 , pyrimidine 16 , 1,2,4-triazine 17,18 ) with adjacent diaryl containing sulfamoyl (SO 2 NH 2 ) or methylsulfonyl (SO 2 Me) substitution at position-4 of one ring which exist in celecoxib, SC-558 and etoricoxib.…”
Section: Introductionmentioning
confidence: 99%
“…Recent studies have also shown that selective COX-2 inhibitors may slow the progress of Alzheimer's disease without causing gastrointestinal damage (Nivsarkar et al, 2008). 1,2-Diarylheterocycles have been extensively studied as selective COX-2 inhibitors (Ghodsi et al, 2010;Penning et al,1997;Prasit et al, 1999;Riendeau et al, 2002;Navidpour et al, 2006;Salimi et al, 2007;Zarghi et al, 2009). All these tricyclic molecules possess 1,2-diaryl substitution on a central hetero or carbocyclic ring system (Fig.…”
Section: Introductionmentioning
confidence: 99%
“…Recently, we reported a group of new diarylheterocyclic COX-2 inhibitors possessing a bicyclic central ring which exhibited highly selectivity for COX-2 inhibition. (Ghodsi et al, 2010;Zarghi et al, 2009). As part of our ongoing program to design new types of tricyclic selective COX-2 inhibitors, we now report the design, synthesis, cyclooxygenase inhibitory, and some molecular modeling studies of a new group of 1,2-diarylheterocycles possessing a 4,5,6,7-tetrahydro-1H-benzo[d]imidazole central ring and a COX-2 SO 2 Me pharmacophore at the para-position of C-2 phenyl ring.…”
Section: Introductionmentioning
confidence: 99%