Page last updated: 2024-08-07 16:13:47
Prostaglandin G/H synthase 1
A prostaglandin G/H synthase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P23219]
Synonyms
EC 1.14.99.1;
Cyclooxygenase-1;
COX-1;
Prostaglandin H2 synthase 1;
PGH synthase 1;
PGHS-1;
PHS 1;
Prostaglandin-endoperoxide synthase 1
Research
Bioassay Publications (192)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 5 (2.60) | 18.7374 |
| 1990's | 35 (18.23) | 18.2507 |
| 2000's | 68 (35.42) | 29.6817 |
| 2010's | 66 (34.38) | 24.3611 |
| 2020's | 18 (9.38) | 2.80 |
Compounds (173)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| salicylic acid | Homo sapiens (human) | IC50 | 270.0000 | 2 | 2 |
| acetaminophen | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| aspirin | Homo sapiens (human) | IC50 | 337.1452 | 10 | 9 |
| aspirin | Homo sapiens (human) | Ki | 62.0000 | 1 | 1 |
| carprofen | Homo sapiens (human) | IC50 | 13.2000 | 1 | 1 |
| celecoxib | Homo sapiens (human) | IC50 | 21.9256 | 71 | 78 |
| diclofenac | Homo sapiens (human) | IC50 | 1.5572 | 12 | 11 |
| dup 697 | Homo sapiens (human) | IC50 | 5.8478 | 5 | 6 |
| etodolac | Homo sapiens (human) | IC50 | 2.6490 | 1 | 0 |
| 4-biphenylylacetic acid | Homo sapiens (human) | IC50 | 0.8940 | 1 | 0 |
| fenoprofen | Homo sapiens (human) | IC50 | 0.1450 | 1 | 0 |
| flufenamic acid | Homo sapiens (human) | IC50 | 2.6150 | 2 | 2 |
| fluoxetine | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| flurbiprofen | Homo sapiens (human) | IC50 | 0.6754 | 3 | 2 |
| ibuprofen | Homo sapiens (human) | IC50 | 7.9035 | 11 | 12 |
| indomethacin | Homo sapiens (human) | IC50 | 1.0591 | 57 | 61 |
| ipriflavone | Homo sapiens (human) | IC50 | 2.9443 | 1 | 0 |
| ketoprofen | Homo sapiens (human) | IC50 | 0.0080 | 2 | 1 |
| ketorolac | Homo sapiens (human) | IC50 | 0.0130 | 1 | 0 |
| loxoprofen | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ly 171883 | Homo sapiens (human) | IC50 | 44.0000 | 1 | 1 |
| meclofenamic acid | Homo sapiens (human) | IC50 | 0.2115 | 2 | 1 |
| mefenamic acid | Homo sapiens (human) | IC50 | 12.5580 | 2 | 1 |
| milrinone | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
| mofezolac | Homo sapiens (human) | IC50 | 0.0036 | 3 | 3 |
| lm 4108 | Homo sapiens (human) | IC50 | 66.0000 | 1 | 1 |
| niflumic acid | Homo sapiens (human) | IC50 | 1.0640 | 1 | 0 |
| nimesulide | Homo sapiens (human) | IC50 | 30.5732 | 7 | 7 |
| nisoxetine | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | Homo sapiens (human) | IC50 | 88.8333 | 5 | 6 |
| oxaprozin | Homo sapiens (human) | IC50 | 0.7980 | 2 | 1 |
| pd 98059 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| propofol | Homo sapiens (human) | IC50 | 3.8320 | 1 | 0 |
| pf 5901 | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
| rofecoxib | Homo sapiens (human) | IC50 | 84.4618 | 23 | 26 |
| rolipram | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sulfinpyrazone | Homo sapiens (human) | IC50 | 509.1000 | 1 | 1 |
| tolmetin | Homo sapiens (human) | IC50 | 0.0410 | 1 | 0 |
| n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | IC50 | 0.2600 | 1 | 0 |
| 2-anisidine | Homo sapiens (human) | IC50 | 3.1520 | 1 | 0 |
| phenidone | Homo sapiens (human) | IC50 | 94.0000 | 1 | 3 |
| phenothiazine | Homo sapiens (human) | IC50 | 0.1960 | 1 | 0 |
| acetyleugenol | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| monobenzone | Homo sapiens (human) | IC50 | 1.0190 | 1 | 0 |
| catechin | Homo sapiens (human) | IC50 | 58.3500 | 2 | 2 |
| osthol | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| carvacrol | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| oleanolic acid | Homo sapiens (human) | IC50 | 380.0000 | 2 | 2 |
| 3,3',4',5-tetrachlorosalicylanilide | Homo sapiens (human) | IC50 | 0.6660 | 1 | 0 |
| tribromsalan | Homo sapiens (human) | IC50 | 2.0650 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 10.3190 | 1 | 0 |
| 6-methoxy-2-naphthylacetic acid | Homo sapiens (human) | IC50 | 4.1130 | 1 | 0 |
| dexibuprofen | Homo sapiens (human) | IC50 | 0.9346 | 3 | 2 |
| 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid | Homo sapiens (human) | IC50 | 0.1300 | 1 | 1 |
| captopril | Homo sapiens (human) | Ki | 17.0000 | 1 | 1 |
| bw-755c | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| atomoxetine | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| mifepristone | Homo sapiens (human) | IC50 | 0.0078 | 1 | 1 |
| pirmagrel | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| zileuton | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tebufelone | Homo sapiens (human) | IC50 | 0.2500 | 3 | 3 |
| tenidap | Homo sapiens (human) | IC50 | 0.0550 | 1 | 0 |
| bromfenac | Homo sapiens (human) | IC50 | 0.0085 | 1 | 0 |
| fenofibric acid | Homo sapiens (human) | IC50 | 950.0000 | 1 | 1 |
| ursolic acid | Homo sapiens (human) | IC50 | 210.0000 | 1 | 1 |
| gallocatechol | Homo sapiens (human) | IC50 | 95.0000 | 1 | 1 |
| rutecarpine | Homo sapiens (human) | IC50 | 8.7000 | 2 | 2 |
| flosulide | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| romazarit | Homo sapiens (human) | IC50 | 6,500.0000 | 1 | 1 |
| clobuzarit | Homo sapiens (human) | IC50 | 950.0000 | 1 | 1 |
| prifelone | Homo sapiens (human) | IC50 | 0.2528 | 2 | 2 |
| sori 8895 | Homo sapiens (human) | IC50 | 0.0460 | 1 | 1 |
| sori 8890 | Homo sapiens (human) | IC50 | 0.0229 | 1 | 1 |
| fangchinoline | Homo sapiens (human) | IC50 | 129.0000 | 1 | 1 |
| n-acetyldopamine | Homo sapiens (human) | IC50 | 18.9000 | 1 | 1 |
| sc 58125 | Homo sapiens (human) | IC50 | 429.0000 | 6 | 8 |
| valdecoxib | Homo sapiens (human) | IC50 | 128.3333 | 5 | 6 |
| mk 0663 | Homo sapiens (human) | IC50 | 62.4000 | 5 | 5 |
| 3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2(5h)-furanone | Homo sapiens (human) | IC50 | 54.3333 | 3 | 3 |
| cyanidin | Homo sapiens (human) | IC50 | 90,000.0000 | 2 | 2 |
| bwa 137c | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| ici d2138 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ml-3000 | Homo sapiens (human) | IC50 | 2.7425 | 4 | 4 |
| cox 189 | Homo sapiens (human) | IC50 | 5.0035 | 2 | 2 |
| enkephalin-leu, des-tyr(1)- | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| atractylenolide iii | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| naproxen | Homo sapiens (human) | IC50 | 7.5102 | 6 | 5 |
| jte 522 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| rhodioloside | Homo sapiens (human) | IC50 | 72.0000 | 1 | 1 |
| cussonoside b | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| cussonoside a | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | IC50 | 3.5000 | 2 | 2 |
| 4'-o-methylepigallocatechin | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| moracin m | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| o-(4-ethoxybutyl)berbamine | Homo sapiens (human) | IC50 | 0.3500 | 1 | 1 |
| fr 122047 | Homo sapiens (human) | IC50 | 0.0590 | 2 | 2 |
| firocoxib | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| cimicoxib | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| berbamine | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| linezolid | Homo sapiens (human) | IC50 | 8.1900 | 1 | 1 |
| dihydropinosylvin | Homo sapiens (human) | IC50 | 46.7000 | 1 | 1 |
| gingerol | Homo sapiens (human) | IC50 | 129.0000 | 1 | 1 |
| e 3040 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sc 57666 | Homo sapiens (human) | IC50 | 455.7143 | 6 | 7 |
| epiafzelechin | Homo sapiens (human) | IC50 | 10.7000 | 2 | 2 |
| resveratrol | Homo sapiens (human) | IC50 | 49.5138 | 4 | 3 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 5.6000 | 1 | 0 |
| kazinol b | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pallidol | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| sinapinic acid | Homo sapiens (human) | IC50 | 39.2000 | 1 | 1 |
| mercaptopurine | Homo sapiens (human) | IC50 | 16.2420 | 1 | 0 |
| dexketoprofen | Homo sapiens (human) | IC50 | 0.0028 | 2 | 2 |
| caffeic acid | Homo sapiens (human) | IC50 | 400.0000 | 1 | 1 |
| capsaicin | Homo sapiens (human) | IC50 | 2.6755 | 2 | 1 |
| enclomiphene | Homo sapiens (human) | IC50 | 0.3460 | 1 | 0 |
| thioguanine anhydrous | Homo sapiens (human) | IC50 | 0.6010 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 4.3910 | 1 | 0 |
| deracoxib | Homo sapiens (human) | IC50 | 31.6667 | 2 | 3 |
| atractylon | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| 1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sc 560 | Homo sapiens (human) | IC50 | 0.0301 | 8 | 9 |
| fraxetin | Homo sapiens (human) | IC50 | 524.0000 | 1 | 1 |
| dinoprost | Homo sapiens (human) | IC50 | 0.1400 | 1 | 1 |
| coniferin | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| linoleic acid | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| daphnetin | Homo sapiens (human) | IC50 | 140.0000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| alpha-linolenic acid | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| genistein | Homo sapiens (human) | IC50 | 80.0000 | 1 | 1 |
| esculetin | Homo sapiens (human) | IC50 | 57.0000 | 1 | 1 |
| morusin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| trans-2,3',4,5'-tetrahydroxystilbene | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| pterostilbene | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| caffeic acid phenethyl ester | Homo sapiens (human) | IC50 | 29.4165 | 2 | 1 |
| beta-funaltrexamine | Homo sapiens (human) | IC50 | 0.0820 | 1 | 1 |
| syringin | Homo sapiens (human) | IC50 | 36.0000 | 1 | 1 |
| osthenol | Homo sapiens (human) | IC50 | 64.0000 | 1 | 1 |
| atractylenolide i | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| sulindac sulfide | Homo sapiens (human) | IC50 | 0.4015 | 2 | 1 |
| gamma-mangostin | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| Norartocarpetin | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
| myricetin 3-o-glucuronide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 3,4-dihydroxy-xanthone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 3,5-dihydroxy-4'-methoxystilbene | Homo sapiens (human) | IC50 | 25.8000 | 1 | 1 |
| bwa 4c | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| kme 4 | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| enofelast | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
| am 404 | Homo sapiens (human) | Ki | 1.5000 | 1 | 1 |
| jwh-133 | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| l 745337 | Homo sapiens (human) | IC50 | 34.3200 | 4 | 5 |
| gw406381x | Homo sapiens (human) | IC50 | 84.2000 | 1 | 1 |
| 4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide | Homo sapiens (human) | IC50 | 25.5000 | 2 | 3 |
| sc-75416 | Homo sapiens (human) | IC50 | 1.0200 | 1 | 1 |
| sch 527123 | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| sc 236 | Homo sapiens (human) | IC50 | 22.3333 | 2 | 3 |
| fk 881 | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| 5-hydroxyrofecoxib | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| delta-viniferin | Homo sapiens (human) | IC50 | 15.1500 | 2 | 2 |
| N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide | Homo sapiens (human) | Ki | 5.4000 | 1 | 1 |
| n-salicyloyltryptamine | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| mk-8141 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| atractylenolide ii | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Norartocarpanone | Homo sapiens (human) | IC50 | 5.9000 | 1 | 1 |
| cauloside D | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tofisopam | Homo sapiens (human) | IC50 | 24.0000 | 1 | 1 |
| kuraridin | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| gnaphalin | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| myrtucommulone a | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| piroxicam | Homo sapiens (human) | IC50 | 68.7254 | 3 | 4 |
| mobic | Homo sapiens (human) | IC50 | 19.9556 | 7 | 9 |
| mobiflex | Homo sapiens (human) | IC50 | 1.1400 | 1 | 0 |
| pf 9184 | Homo sapiens (human) | IC50 | 118.0000 | 1 | 1 |
| sildenafil | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| celecoxib | Homo sapiens (human) | Inhibition | 15.0000 | 1 | 1 |
| phenidone | Homo sapiens (human) | Activity | 300.0000 | 1 | 1 |
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.European journal of medicinal chemistry, , May-01, Volume: 193, 2020
Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
N-Caffeoyl serotonin as selective COX-2 inhibitor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 22, Issue:7, 2012
Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 2011
3-Formylchromones: potential antiinflammatory agents.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.Journal of natural products, , Volume: 70, Issue:5, 2007
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.Journal of natural products, , Volume: 62, Issue:2, 1999
Benzimidazole derivatives with atypical antiinflammatory activity.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
[no title available],
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 33, 2021
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 30, Issue:17, 2020
Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.European journal of medicinal chemistry, , Nov-01, Volume: 205, 2020
New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.MedChemComm, , Oct-01, Volume: 10, Issue:10, 2019
Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.European journal of medicinal chemistry, , May-01, Volume: 169, 2019
Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 29, Issue:15, 2019
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 27, Issue:16, 2017
[no title available]Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 27, Issue:4, 2017
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression.European journal of medicinal chemistry, , Jun-23, Volume: 81, 2014
Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Synthesis of novel 1,2,3-triazole based benzoxazolinones: their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation.European journal of medicinal chemistry, , Volume: 70, 2013
Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and -2-alkylsulfonyl-1H-imidazole derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.European journal of medicinal chemistry, , Volume: 62, 2013
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 20, Issue:22, 2012
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Structure-based parallel medicinal chemistry approach to improve metabolic stability of benzopyran COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Synthesis and biological evaluation of loxoprofen derivatives.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.Journal of enzyme inhibition and medicinal chemistry, , Volume: 24, Issue:1, 2009
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.European journal of medicinal chemistry, , Volume: 43, Issue:3, 2008
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.Journal of natural products, , Volume: 68, Issue:10, 2005
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
[no title available],
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Exploring activity cliffs in medicinal chemistry.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Toward optimization of the second aryl substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.Journal of natural products, , Volume: 68, Issue:10, 2005
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
[no title available],
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
[no title available]Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Synthesis, COX-1/2 inhibition activities and molecular docking study of isothiazolopyridine derivatives.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
[no title available],
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Sila-Ibuprofen.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.Journal of natural products, , Volume: 62, Issue:2, 1999
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
[no title available],
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.Bioorganic & medicinal chemistry, , 01-15, Volume: 28, Issue:2, 2020
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Synthesis and biological evaluation of pyridazinone derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery.Bioorganic & medicinal chemistry, , 07-30, Volume: 26, Issue:13, 2018
Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 27, Issue:4, 2017
Synthesis and characterization of novel oxazines and demonstration that they specifically target cyclooxygenase 2.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.Journal of medicinal chemistry, , Mar-28, Volume: 56, Issue:6, 2013
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 22, Issue:13, 2012
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Bioactive sulfoximines: syntheses and properties of Vioxx analogs.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 2011
Pyrazol-3-propanoic acid derivatives as novel inhibitors of leukotriene biosynthesis in human neutrophils.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
3-Formylchromones: potential antiinflammatory agents.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Synthesis and biological evaluation of some thiazolylpyrazole derivatives as dual anti-inflammatory antimicrobial agents.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.Journal of enzyme inhibition and medicinal chemistry, , Volume: 24, Issue:1, 2009
The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Synthesis and evaluation of dithiolethiones as novel cyclooxygenase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Synthesis and biological evaluation of some thiazolyl and thiadiazolyl derivatives of 1H-pyrazole as anti-inflammatory antimicrobial agents.European journal of medicinal chemistry, , Volume: 43, Issue:3, 2008
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.Journal of natural products, , Volume: 70, Issue:5, 2007
Quercinol, an anti-inflammatory chromene from the wood-rotting fungus Daedalea quercina (Oak Mazegill).Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
5-Lipoxygenase and cyclooxygenase-1 inhibitory active compounds from Atractylodes lancea.Journal of natural products, , Volume: 61, Issue:3, 1998
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents.Journal of medicinal chemistry, , May-23, Volume: 40, Issue:11, 1997
Novel terphenyls as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Benzimidazole derivatives with atypical antiinflammatory activity.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
[no title available],
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
In vitro antiproliferative activity against human colon cancer cell lines of representative 4-thiazolidinones. Part I.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
[no title available],
Synthesis and PGE₂ production inhibition of s-triazine derivatives as a novel scaffold in RAW 264.7 macrophage cells.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor.Bioorganic & medicinal chemistry letters, , Mar-11, Volume: 12, Issue:5, 2002
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , May-19, Volume: 13, Issue:10, 2003
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.Journal of medicinal chemistry, , Jul-31, Volume: 46, Issue:16, 2003
Synthesis and structure-activity relationship of novel, highly potent metharyl and methcycloalkyl cyclooxygenase-2 (COX-2) selective inhibitors.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1)Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Isomeric acetoxy analogues of rofecoxib: a novel class of highly potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor.Bioorganic & medicinal chemistry letters, , Mar-11, Volume: 12, Issue:5, 2002
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).Bioorganic & medicinal chemistry letters, , Dec-04, Volume: 10, Issue:23, 2000
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
[no title available],
A facile synthesis of 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, a selective 15-lipoxygenase inhibitor.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Recent developments in fragment-based drug discovery.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
[no title available],
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Analogue-based design, synthesis and docking of non-steroidal anti-inflammatory agents. Part 2: methyl sulfanyl/methyl sulfonyl substituted 2,3-diaryl-2,3-dihydro-1H-quinazolin-4-ones.Bioorganic & medicinal chemistry, , Dec-15, Volume: 20, Issue:24, 2012
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Effect of structure on potency and selectivity in 2,6-disubstituted 4-(2-arylethenyl)phenol lipoxygenase inhibitors.Journal of medicinal chemistry, , Volume: 33, Issue:7, 1990
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Novel valdecoxib derivatives by ruthenium(ii)-promoted 1,3-dipolar cycloaddition of nitrile oxides with alkynes - synthesis and COX-2 inhibition activity.MedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.Journal of natural products, , Volume: 62, Issue:2, 1999
Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.European journal of medicinal chemistry, , Mar-01, Volume: 189, 2020
Inhibition of the enzymes in the leukotriene and prostaglandin pathways in inflammation by 3-aryl isocoumarins.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
(6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase.Journal of medicinal chemistry, , Jun-10, Volume: 37, Issue:12, 1994
Exploring activity cliffs in medicinal chemistry.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Jan-27, Volume: 43, Issue:2, 2000
Antioxidant and antiinflammatory activities of anthocyanins and their aglycon, cyanidin, from tart cherries.Journal of natural products, , Volume: 62, Issue:2, 1999
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
[no title available],
Kinase inhibitors: not just for kinases anymore.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Diarylspiro[2.4]heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Synthesis and biological evaluation of a library of resveratrol analogues as inhibitors of COX-1, COX-2 and NF-kappaB.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Constituents of the bark and twigs of Artocarpus dadah with cyclooxygenase inhibitory activity.Journal of natural products, , Volume: 65, Issue:2, 2002
[no title available],
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
[no title available]Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Synthesis, cyclooxygenase inhibitory effects, and molecular modeling study of 4-aryl-5-(4-(methylsulfonyl)phenyl)-2-alkylthio and -2-alkylsulfonyl-1H-imidazole derivatives.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Design, synthesis and pharmacobiological evaluation of novel acrylic acid derivatives acting as lipoxygenase and cyclooxygenase-1 inhibitors with antioxidant and anti-inflammatory activities.European journal of medicinal chemistry, , Volume: 46, Issue:1, 2011
Triterpene saponins from Clematis chinensis and their potential anti-inflammatory activity.Journal of natural products, , Jul-23, Volume: 73, Issue:7, 2010
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class.Bioorganic & medicinal chemistry letters, , Jan-18, Volume: 9, Issue:2, 1999
1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters, , May-13, Volume: 12, Issue:5, 2021
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Constituents of the bark and twigs of Artocarpus dadah with cyclooxygenase inhibitory activity.Journal of natural products, , Volume: 65, Issue:2, 2002
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).Journal of medicinal chemistry, , Apr-25, Volume: 40, Issue:9, 1997
Synthesis, COX-1/2 inhibition activities and molecular docking study of isothiazolopyridine derivatives.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
[no title available],
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
[no title available]Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
COX-1/COX-2 inhibition activities and molecular docking study of newly designed and synthesized pyrrolo[3,4-c]pyrrole Mannich bases.Bioorganic & medicinal chemistry, , 09-01, Volume: 27, Issue:17, 2019
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: novel inhibitors of COX-2.Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, Issue:10, 1998
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
[no title available],
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| peroxidase activity | molecular function | Catalysis of the reaction: a donor + a peroxide = an oxidized donor + 2 H2O. [GOC:curators] |
| prostaglandin-endoperoxide synthase activity | molecular function | Catalysis of the reaction: arachidonate + donor-H2 + 2 O2 = prostaglandin H2 + acceptor + H2O. [EC:1.14.99.1] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen | molecular function | Catalysis of an oxidation-reduction (redox) reaction in which hydrogen or electrons are transferred from one donor, and two oxygen atoms is incorporated into a donor. [GOC:mah] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| photoreceptor outer segment | cellular component | The outer segment of a vertebrate photoreceptor that contains a stack of membrane discs embedded with photoreceptor proteins. [GOC:cilia, GOC:krc, GOC:pde, ISBN:0824072820, PMID:19501669, PMID:26574505, PMID:6771304] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|
| prostaglandin biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of prostaglandins, any of a group of biologically active metabolites which contain a cyclopentane ring. [GOC:ai] |
| response to oxidative stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| cyclooxygenase pathway | biological process | The chemical reactions and pathways by which prostaglandins are formed from arachidonic acid, and in which prostaglandin-endoperoxide synthase (cyclooxygenase) catalyzes the committed step in the conversion of arachidonic acid to the prostaglandin-endoperoxides PGG2 and PGH2. [PMID:19854273] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| cellular oxidant detoxification | biological process | Any process carried out at the cellular level that reduces or removes the toxicity superoxide radicals or hydrogen peroxide. [GOC:dos, GOC:vw] |