Page last updated: 2024-08-07 16:33:26
Prostaglandin G/H synthase 2
A prostaglandin G/H synthase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P35354]
Synonyms
EC 1.14.99.1;
Cyclooxygenase-2;
COX-2;
PHS II;
Prostaglandin H2 synthase 2;
PGH synthase 2;
PGHS-2;
Prostaglandin-endoperoxide synthase 2
Research
Bioassay Publications (338)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 5 (1.48) | 18.7374 |
| 1990's | 39 (11.54) | 18.2507 |
| 2000's | 86 (25.44) | 29.6817 |
| 2010's | 174 (51.48) | 24.3611 |
| 2020's | 34 (10.06) | 2.80 |
Compounds (281)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| salicylic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| digallic acid | Homo sapiens (human) | Ki | 0.3900 | 1 | 1 |
| pyrogallol | Homo sapiens (human) | IC50 | 144.0000 | 1 | 1 |
| 2-(6-methoxy-2-naphthalenyl)propanoic acid | Homo sapiens (human) | IC50 | 0.2800 | 1 | 1 |
| ampyrone | Homo sapiens (human) | IC50 | 42.0000 | 1 | 1 |
| n'-(3-aminopropyl)homospermidine | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| aspirin | Homo sapiens (human) | IC50 | 907.5235 | 24 | 26 |
| aspirin | Homo sapiens (human) | Ki | 52.0000 | 1 | 1 |
| bml 190 | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| carprofen | Homo sapiens (human) | IC50 | 1.0510 | 4 | 4 |
| celecoxib | Homo sapiens (human) | IC50 | 4.1281 | 167 | 174 |
| celecoxib | Homo sapiens (human) | Ki | 0.0005 | 1 | 2 |
| cisapride | Homo sapiens (human) | IC50 | 3.3700 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 41.7960 | 1 | 0 |
| diclofenac | Homo sapiens (human) | IC50 | 3.2751 | 22 | 21 |
| dup 697 | Homo sapiens (human) | IC50 | 5.8107 | 17 | 22 |
| etodolac | Homo sapiens (human) | IC50 | 0.5610 | 1 | 0 |
| flufenamic acid | Homo sapiens (human) | IC50 | 3.1120 | 3 | 3 |
| flurbiprofen | Homo sapiens (human) | IC50 | 0.5740 | 5 | 5 |
| hexachlorophene | Homo sapiens (human) | IC50 | 0.6443 | 1 | 0 |
| ibuprofen | Homo sapiens (human) | IC50 | 39.6996 | 35 | 36 |
| indomethacin | Homo sapiens (human) | IC50 | 8.1537 | 95 | 107 |
| indomethacin | Homo sapiens (human) | Ki | 1.5000 | 1 | 1 |
| ketoprofen | Homo sapiens (human) | IC50 | 1.1680 | 4 | 3 |
| ketorolac | Homo sapiens (human) | IC50 | 0.2820 | 2 | 1 |
| 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 | 0.1618 | 4 | 5 |
| mefenamic acid | Homo sapiens (human) | IC50 | 1.7510 | 2 | 1 |
| mesalamine | Homo sapiens (human) | IC50 | 7.5300 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 25.8440 | 1 | 0 |
| mofezolac | Homo sapiens (human) | IC50 | 30.1760 | 5 | 5 |
| lm 4108 | Homo sapiens (human) | IC50 | 13.2880 | 3 | 5 |
| niflumic acid | Homo sapiens (human) | IC50 | 0.9180 | 1 | 0 |
| nimesulide | Homo sapiens (human) | IC50 | 26.9698 | 10 | 9 |
| masoprocol | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | Homo sapiens (human) | IC50 | 12.5632 | 22 | 25 |
| nu6102 | Homo sapiens (human) | IC50 | 0.0081 | 1 | 1 |
| oxaprozin | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| phenylbutazone | Homo sapiens (human) | IC50 | 284.0000 | 1 | 1 |
| pf 5901 | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
| rofecoxib | Homo sapiens (human) | IC50 | 14.6393 | 43 | 44 |
| vorinostat | Homo sapiens (human) | IC50 | 0.1300 | 1 | 1 |
| pirinixic acid | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| prednisolone | Homo sapiens (human) | Ki | 5.0000 | 1 | 2 |
| n,n'-diphenyl-4-phenylenediamine | Homo sapiens (human) | IC50 | 0.5800 | 1 | 0 |
| phenidone | Homo sapiens (human) | IC50 | 94.0000 | 1 | 3 |
| phenothiazine | Homo sapiens (human) | IC50 | 0.5320 | 1 | 0 |
| phenylhydrazine | Homo sapiens (human) | IC50 | 1.5140 | 1 | 0 |
| monobenzone | Homo sapiens (human) | IC50 | 3.7260 | 1 | 0 |
| catechin | Homo sapiens (human) | IC50 | 111.6500 | 2 | 2 |
| glycyrrhetinic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| osthol | Homo sapiens (human) | IC50 | 81.1000 | 1 | 1 |
| olivetol | Homo sapiens (human) | IC50 | 17.2600 | 1 | 1 |
| oleanolic acid | Homo sapiens (human) | IC50 | 179.2500 | 4 | 4 |
| 3,3',4',5-tetrachlorosalicylanilide | Homo sapiens (human) | IC50 | 0.5420 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 2.8620 | 1 | 0 |
| nitroxoline | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| indomethacin ethyl ester | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| dexibuprofen | Homo sapiens (human) | IC50 | 1.5950 | 2 | 2 |
| 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid | Homo sapiens (human) | IC50 | 6.6250 | 2 | 2 |
| closantel | Homo sapiens (human) | IC50 | 1.8390 | 1 | 0 |
| captopril | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| bw-755c | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| lovastatin | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| simvastatin | Homo sapiens (human) | IC50 | 0.0034 | 1 | 0 |
| pravastatin | Homo sapiens (human) | IC50 | 0.0056 | 1 | 0 |
| pirmagrel | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| tepoxalin | Homo sapiens (human) | IC50 | 2.8500 | 1 | 1 |
| zileuton | Homo sapiens (human) | IC50 | 80.0000 | 2 | 2 |
| tebufelone | Homo sapiens (human) | IC50 | 0.1000 | 3 | 3 |
| tenidap | Homo sapiens (human) | IC50 | 0.2670 | 1 | 0 |
| bromfenac | Homo sapiens (human) | IC50 | 0.0048 | 1 | 0 |
| atorvastatin | Homo sapiens (human) | IC50 | 0.0002 | 1 | 0 |
| mevastatin | Homo sapiens (human) | IC50 | 0.1190 | 1 | 0 |
| ursolic acid | Homo sapiens (human) | IC50 | 85.3333 | 3 | 3 |
| medicagenic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| rutecarpine | Homo sapiens (human) | IC50 | 0.2900 | 2 | 2 |
| isoscopoletin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| flosulide | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
| romazarit | Homo sapiens (human) | IC50 | 6,500.0000 | 1 | 1 |
| masoprocol | Homo sapiens (human) | IC50 | 6.7500 | 1 | 2 |
| clobuzarit | Homo sapiens (human) | IC50 | 950.0000 | 1 | 1 |
| prifelone | Homo sapiens (human) | IC50 | 0.2528 | 2 | 2 |
| (S)-flurbiprofen | Homo sapiens (human) | IC50 | 0.9100 | 1 | 1 |
| avarol | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
| tryptanthrine | Homo sapiens (human) | IC50 | 0.0640 | 3 | 3 |
| arjunolic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| maslinic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| adipostatin a | Homo sapiens (human) | IC50 | 2.3600 | 1 | 1 |
| ketorolac tromethamine | Homo sapiens (human) | IC50 | 30.3100 | 2 | 2 |
| primin | Homo sapiens (human) | IC50 | 1.9000 | 1 | 1 |
| tarenflurbil | Homo sapiens (human) | IC50 | 123.0000 | 1 | 1 |
| triptolide | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
| parthenolide | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| sc 58125 | Homo sapiens (human) | IC50 | 0.2316 | 10 | 10 |
| asiatic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| valdecoxib | Homo sapiens (human) | IC50 | 0.0631 | 11 | 10 |
| parecoxib | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| mk 0663 | Homo sapiens (human) | IC50 | 0.4586 | 8 | 9 |
| mk 0663 | Homo sapiens (human) | Ki | 0.0690 | 1 | 2 |
| 3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2(5h)-furanone | Homo sapiens (human) | IC50 | 0.3867 | 3 | 3 |
| cyanidin | Homo sapiens (human) | IC50 | 60,000.0000 | 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 | 8.8729 | 7 | 7 |
| cox 189 | Homo sapiens (human) | IC50 | 2.0608 | 5 | 5 |
| cox 189 | Homo sapiens (human) | Ki | 0.3200 | 1 | 1 |
| enkephalin-leu, des-tyr(1)- | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| naproxen | Homo sapiens (human) | IC50 | 104.4055 | 11 | 10 |
| jte 522 | Homo sapiens (human) | IC50 | 0.0850 | 1 | 1 |
| boswellic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| cussonoside b | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| cussonoside a | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| moracin m | Homo sapiens (human) | IC50 | 22.3000 | 1 | 1 |
| fr 122047 | Homo sapiens (human) | IC50 | 65.0000 | 1 | 1 |
| cimicoxib | Homo sapiens (human) | IC50 | 0.0367 | 3 | 3 |
| tenulin | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| dihydropinosylvin | Homo sapiens (human) | IC50 | 46.7000 | 1 | 1 |
| gingerol | Homo sapiens (human) | IC50 | 125.0000 | 1 | 1 |
| e 3040 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sc 57666 | Homo sapiens (human) | IC50 | 0.1258 | 8 | 8 |
| epiafzelechin | Homo sapiens (human) | IC50 | 69.7000 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 6.0046 | 7 | 7 |
| cerivastatin | Homo sapiens (human) | IC50 | 0.0001 | 1 | 0 |
| kazinol b | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pallidol | Homo sapiens (human) | IC50 | 80.0000 | 1 | 1 |
| tolfenamic acid | Homo sapiens (human) | IC50 | 0.8800 | 1 | 1 |
| boswellic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| cinnamaldehyde | Homo sapiens (human) | IC50 | 245.0000 | 1 | 1 |
| sinapinic acid | Homo sapiens (human) | IC50 | 28.0000 | 1 | 1 |
| propolin c | Homo sapiens (human) | IC50 | 4.2000 | 1 | 1 |
| dexketoprofen | Homo sapiens (human) | IC50 | 0.1285 | 2 | 1 |
| caffeic acid | Homo sapiens (human) | IC50 | 66.3500 | 2 | 2 |
| 2-hydroxy-5-[[(5-methyl-2-furanyl)-oxomethyl]amino]benzoic acid | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| curcumin | Homo sapiens (human) | IC50 | 63.8350 | 1 | 2 |
| urb 597 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sulindac | Homo sapiens (human) | IC50 | 8.8000 | 1 | 1 |
| deracoxib | Homo sapiens (human) | IC50 | 0.0501 | 2 | 2 |
| l 663536 | Homo sapiens (human) | IC50 | 15.7025 | 3 | 4 |
| 1-phenyl-2-[[4-(trifluoromethyl)phenyl]methylthio]imidazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| sc 560 | Homo sapiens (human) | IC50 | 21.5994 | 7 | 7 |
| diclofenac sodium | Homo sapiens (human) | IC50 | 0.8200 | 6 | 6 |
| quercetin | Homo sapiens (human) | IC50 | 28.6000 | 1 | 1 |
| dinoprost | Homo sapiens (human) | IC50 | 0.1400 | 1 | 1 |
| apigenin | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| scopoletin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 150.0000 | 1 | 1 |
| chrysin | Homo sapiens (human) | IC50 | 25.5000 | 1 | 1 |
| morusin | Homo sapiens (human) | IC50 | 100.0000 | 2 | 2 |
| wogonin | Homo sapiens (human) | IC50 | 34.8650 | 4 | 4 |
| trans-2,3',4,5'-tetrahydroxystilbene | Homo sapiens (human) | IC50 | 109.0000 | 1 | 1 |
| pterostilbene | Homo sapiens (human) | IC50 | 0.8200 | 1 | 1 |
| caffeic acid phenethyl ester | Homo sapiens (human) | IC50 | 82.0000 | 1 | 1 |
| bisdemethoxycurcumin | Homo sapiens (human) | IC50 | 36.3700 | 1 | 1 |
| muromonab-cd3 | Homo sapiens (human) | IC50 | 2.5000 | 1 | 1 |
| angiotensin amide | Homo sapiens (human) | IC50 | 4.6000 | 1 | 1 |
| sulindac sulfide | Homo sapiens (human) | IC50 | 0.9182 | 4 | 3 |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid | Homo sapiens (human) | IC50 | 0.0004 | 1 | 0 |
| ajoene | Homo sapiens (human) | IC50 | 3.4000 | 1 | 1 |
| 3,4',5-trimethoxystilbene | Homo sapiens (human) | IC50 | 1.6670 | 1 | 1 |
| gamma-mangostin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 4',7,8-trihydroxyisoflavone | Homo sapiens (human) | IC50 | 150.0000 | 1 | 2 |
| Norartocarpetin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| myricetin 3-o-glucuronide | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| mimulone | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| 3,4-dihydroxy-xanthone | Homo sapiens (human) | IC50 | 1.8900 | 1 | 1 |
| 3,5-dihydroxy-4'-methoxystilbene | Homo sapiens (human) | IC50 | 19.6000 | 1 | 1 |
| monorden | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
| bwa 4c | Homo sapiens (human) | IC50 | 1.6050 | 2 | 2 |
| kme 4 | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
| enofelast | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
| ci 987 | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
| s 1360 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| corosolic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| l 745337 | Homo sapiens (human) | IC50 | 0.0530 | 4 | 4 |
| gw406381x | Homo sapiens (human) | IC50 | 0.0030 | 2 | 2 |
| 4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide | Homo sapiens (human) | IC50 | 0.0409 | 4 | 5 |
| 11-keto-boswellic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| sc-75416 | Homo sapiens (human) | IC50 | 0.0620 | 1 | 1 |
| sc 236 | Homo sapiens (human) | IC50 | 0.0081 | 4 | 5 |
| fk 881 | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| 5-hydroxyrofecoxib | Homo sapiens (human) | IC50 | 8.7000 | 1 | 1 |
| arachidonoylserotonin | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| delta-viniferin | Homo sapiens (human) | IC50 | 3.7000 | 1 | 1 |
| cay 10404 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| amg 009 | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
| acetyl-11-ketoboswellic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 3-o-acetyl-beta-boswellic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 11-deoxy glycyrrhetinic acid | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| alpha-amyrenone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| roburic acid | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| 4-(4-(3-adamantan-1-ylureido)cyclohexyloxy)benzoic acid | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| tannins | Homo sapiens (human) | IC50 | 3.1270 | 1 | 0 |
| Norartocarpanone | Homo sapiens (human) | IC50 | 46.4000 | 1 | 1 |
| cauloside D | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| tofisopam | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| beta-Elemonic acid | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ys 121 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| amg 853 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| N-[(5-bromo-8-hydroxy-7-quinolinyl)-thiophen-2-ylmethyl]acetamide | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| piroxicam | Homo sapiens (human) | IC50 | 136.6417 | 2 | 3 |
| mobic | Homo sapiens (human) | IC50 | 8.5598 | 7 | 6 |
| pf 9184 | Homo sapiens (human) | IC50 | 154.3333 | 3 | 3 |
| cep-28122 | Homo sapiens (human) | IC50 | 0.0019 | 1 | 1 |
| sildenafil | Homo sapiens (human) | IC50 | 0.0030 | 1 | 1 |
| hydrazinocurcumin | Homo sapiens (human) | IC50 | 9.7000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
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
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.Bioorganic chemistry, , Volume: 63, 2015
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Enzymatic Studies of Isoflavonoids as Selective and Potent Inhibitors of Human Leukocyte 5-Lipo-Oxygenase.Chemical biology & drug design, , Volume: 86, Issue:1, 2015
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
N-Caffeoyl serotonin as selective COX-2 inhibitor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 22, Issue:7, 2012
Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 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
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
3-Formylchromones: potential antiinflammatory agents.European journal of medicinal chemistry, , Volume: 45, Issue:9, 2010
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Synthesis and biological evaluation of salicylic acid and N-acetyl-2-carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory acBioorganic & medicinal chemistry letters, , Dec-15, Volume: 19, Issue:24, 2009
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
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.Journal of natural products, , Volume: 70, Issue:5, 2007
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
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 conformationally constrained aci-reductone mimics of arachidonic acid.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.Journal of medicinal chemistry, , Nov-19, Volume: 41, Issue:24, 1998
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Benzimidazole derivatives with atypical antiinflammatory activity.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
SAR studies of acidic dual γ-secretase/PPARγ modulators.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Perspectives in animal health: old targets and new opportunities.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.Bioorganic & medicinal chemistry, , 03-01, Volume: 57, 2022
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
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
[no title available]European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 222, 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
Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 46, 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 computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential.European journal of medicinal chemistry, , Nov-15, Volume: 224, 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
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
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
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.European journal of medicinal chemistry, , Aug-15, Volume: 200, 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
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.Bioorganic & medicinal chemistry, , 04-01, Volume: 28, Issue:7, 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
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 30, Issue:17, 2020
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.European journal of medicinal chemistry, , Apr-01, Volume: 167, 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
Human disorders associated with inflammation and the evolving role of natural products to overcome.European journal of medicinal chemistry, , Oct-01, Volume: 179, 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
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 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
[no title available]Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Role of sulphur-heterocycles in medicinal chemistry: An update.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES.European journal of medicinal chemistry, , Jun-01, Volume: 171, 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
Synthesis, in vitro and in silico evaluation of novel trans-stilbene analogues as potential COX-2 inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018
Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.Bioorganic & medicinal chemistry, , 02-15, Volume: 26, Issue:4, 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
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives.Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents.Bioorganic chemistry, , Volume: 71, 2017
In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings.Bioorganic chemistry, , Volume: 70, 2017
Novel 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene analogues as selective COX-2 inhibitors: Design, synthesis, anti-inflammatory evaluation, and molecular docking studies.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 27, Issue:8, 2017
Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
[no title available]Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 27, Issue:18, 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
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
Lipid Peroxidation and Cyclooxygenase Enzyme Inhibitory Compounds from Prangos haussknechtii.Journal of natural products, , 09-22, Volume: 80, Issue:9, 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]Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 127, 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
Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).MedChemComm, , Mar-01, Volume: 8, Issue:3, 2017
[no title available]Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
[no title available]Bioorganic chemistry, , Volume: 72, 2017
Structure-activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
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 and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 26, Issue:6, 2016
Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.Bioorganic chemistry, , Volume: 64, 2016
1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.Bioorganic chemistry, , Volume: 63, 2015
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
Five new phorbol esters with cytotoxic and selective anti-inflammatory activities from Croton tiglium.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 25, Issue:24, 2015
Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 25, Issue:16, 2015
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 25, Issue:12, 2015
Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
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
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Synthesis of thio-heterocyclic analogues from Baylis-Hillman bromides as potent cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: design, synthesis and evaluation as potential anti-inflammatory agents.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Benzimidazole: an emerging scaffold for analgesic and anti-inflammatory agents.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
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
Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Design, synthesis, docking and anti-inflammatory evaluation of novel series of benzofuran based prodrugs.Bioorganic & medicinal chemistry letters, , May-15, Volume: 24, Issue:10, 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
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
1,4-Diaryl-substituted triazoles as cyclooxygenase-2 inhibitors: Synthesis, biological evaluation and molecular modeling studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.European journal of medicinal chemistry, , Volume: 62, 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
Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 2012
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
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
Radiosynthesis of a ¹⁸F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Synthesis and evaluation of fluorobenzoylated di- and tripeptides as inhibitors of cyclooxygenase-2 (COX-2).Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Enzymatic transformation of caffeic acid with enhanced cyclooxygenase-2 inhibitory activity.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 2012
Fragment-based design, docking, synthesis, biological evaluation and structure-activity relationships of 2-benzo/benzisothiazolimino-5-aryliden-4-thiazolidinones as cycloxygenase/lipoxygenase inhibitors.European journal of medicinal chemistry, , Volume: 47, Issue:1, 2012
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
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
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
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Synthesis and biological evaluation of loxoprofen derivatives.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 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
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
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
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 of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 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
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
Synthesis of 1-(methanesulfonyl- and aminosulfonylphenyl)acetylenes that possess a 2-(N-difluoromethyl-1,2-dihydropyridin-2-one) pharmacophore: evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 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
Exploration of physicochemical properties and molecular modelling studies of 2-sulfonyl-phenyl-3-phenyl-indole analogs as cyclooxygenase-2 inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:6, 2008
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.European journal of medicinal chemistry, , Volume: 43, Issue:6, 2008
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
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
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
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.Journal of natural products, , Volume: 68, Issue:10, 2005
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 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 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
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
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
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
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Estimation of binding affinities for celecoxib analogues with COX-2 via Monte Carlo-extended linear response.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.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
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
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 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
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
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 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
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
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
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
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
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],
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
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
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
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
Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity.European journal of medicinal chemistry, , Jun-10, Volume: 80, 2014
Exploring activity cliffs in medicinal chemistry.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.The Journal of biological chemistry, , Jun-01, Volume: 282, Issue:22, 2007
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.Journal of natural products, , Volume: 68, Issue:10, 2005
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 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],
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
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
Novel 1,3,4-oxadiazole/oxime hybrids: Synthesis, docking studies and investigation of anti-inflammatory, ulcerogenic liability and analgesic activities.Bioorganic chemistry, , Volume: 69, 2016
Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system.ACS chemical biology, , Jul-18, Volume: 9, Issue:7, 2014
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 isoxazolo[4,5-d]pyridazin-4-(5H)-one analogues as potent anti-inflammatory agents.Bioorganic & medicinal chemistry, , May-01, Volume: 20, Issue:9, 2012
Synthesis and PGE(2) production inhibition of 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
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
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
Structure-based design of COX-2 selectivity into flurbiprofen.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 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
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 and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.European journal of medicinal chemistry, , Volume: 62, 2013
Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Synthesis, COX-1/2 inhibition activities and molecular docking study of isothiazolopyridine derivatives.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Structure-based design of COX-2 selectivity into flurbiprofen.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
[no title available],
Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation.Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Synthesis, Inhibitory Activity, and ACS medicinal chemistry letters, , Apr-08, Volume: 12, Issue:4, 2021
Sila-Ibuprofen.Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Prenylated Stilbenoids Affect Inflammation by Inhibiting the NF-κB/AP-1 Signaling Pathway and Cyclooxygenases and Lipoxygenase.Journal of natural products, , 07-26, Volume: 82, Issue:7, 2019
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.Bioorganic & medicinal chemistry, , 02-15, Volume: 26, Issue:4, 2018
An overview of benzo[b]thiophene-based medicinal chemistry.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Anti-inflammatory Activity of Natural Geranylated Flavonoids: Cyclooxygenase and Lipoxygenase Inhibitory Properties and Proteomic Analysis.Journal of natural products, , 04-28, Volume: 80, Issue:4, 2017
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.Bioorganic chemistry, , Volume: 63, 2015
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Enzymatic Studies of Isoflavonoids as Selective and Potent Inhibitors of Human Leukocyte 5-Lipo-Oxygenase.Chemical biology & drug design, , Volume: 86, Issue:1, 2015
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Binding of ibuprofen, ketorolac, and diclofenac to COX-1 and COX-2 studied by saturation transfer difference NMR.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
SAR studies of acidic dual γ-secretase/PPARγ modulators.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Celecoxib prodrugs possessing a diazen-1-ium-1,2-diolate nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Synthesis and biological evaluation of N-difluoromethyl-1,2-dihydropyrid-2-one acetic acid regioisomers: dual inhibitors of cyclooxygenases and 5-lipoxygenase.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-carboxymethylphenyl)-1-(4-methanesulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its aminosulfonyl analog: Synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Synthesis and biological evaluation of salicylic acid and N-acetyl-2-carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory acBioorganic & medicinal chemistry letters, , Dec-15, Volume: 19, Issue:24, 2009
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 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
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. 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
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
[no title available],
Synthetic methodology-enabled discovery of a tunable indole template for COX-1 inhibition and anti-cancer activity.Bioorganic & medicinal chemistry, , 03-01, Volume: 57, 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
Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Synthesis and computational studies of novel fused pyrimidinones as a promising scaffold with analgesic, anti-inflammatory and COX inhibitory potential.European journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.European journal of medicinal chemistry, , Aug-15, Volume: 200, 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
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.Bioorganic & medicinal chemistry, , 04-01, Volume: 28, Issue:7, 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
Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.European journal of medicinal chemistry, , Apr-01, Volume: 167, 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
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
[no title available]Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.European journal of medicinal chemistry, , Jan-20, Volume: 144, 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
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Tailoring the Substitution Pattern on 1,3,5-Triazine for Targeting Cyclooxygenase-2: Discovery and Structure-Activity Relationship of Triazine-4-Aminophenylmorpholin-3-one Hybrids that Reverse Algesia and Inflammation in Swiss Albino Mice.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents.Bioorganic chemistry, , Volume: 71, 2017
Synthesis, anti-inflammatory, cyclooxygenases inhibitions assays and histopathological study of poly-substituted 1,3,5-triazines: Confirmation of regiospecific pyrazole cyclization by HMBC.European journal of medicinal chemistry, , Feb-15, Volume: 127, 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
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
[no title available]Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
[no title available]Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
1,2-Diaryl-2-hydroxyiminoethanones as dual COX-1 and β-amyloid aggregation inhibitors: biological evaluation and in silico study.Chemical biology & drug design, , Volume: 85, Issue:4, 2015
Synthesis, Molecular Modeling, and Biological Evaluation of Novel 1, 3-Diphenyl-2-propen-1-one Based Pyrazolines as Anti-inflammatory Agents.Chemical biology & drug design, , Volume: 85, Issue:6, 2015
Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
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
Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1.Chemical biology & drug design, , Volume: 83, Issue:6, 2014
1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
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
Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Pharmacological evaluation and docking studies of α,β-unsaturated carbonyl based synthetic compounds as inhibitors of secretory phospholipase A₂, cyclooxygenases, lipoxygenase and proinflammatory cytokines.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor.ACS medicinal chemistry letters, , May-09, Volume: 4, Issue:5, 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
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 22, Issue:21, 2012
Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity.European journal of medicinal chemistry, , Volume: 57, 2012
Nitric oxide release is not required to decrease the ulcerogenic profile of nonsteroidal anti-inflammatory drugs.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
N-1 and C-3 substituted indole Schiff bases as selective COX-2 inhibitors: synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 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
SAR studies of acidic dual γ-secretase/PPARγ modulators.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro.Journal of natural products, , Apr-25, Volume: 74, Issue:4, 2011
Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
Synthesis and evaluation of carbaborane derivatives of indomethacin as cyclooxygenase inhibitors.Bioorganic & medicinal chemistry, , May-15, Volume: 19, Issue:10, 2011
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 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 and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.Journal of medicinal chemistry, , Jun-24, Volume: 53, 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 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
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 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
Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2.Journal of natural products, , Volume: 69, Issue:6, 2006
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
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
Synthesis and cyclooxygenase-2 inhibiting property of 1,5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: Preparation of sodium salt for injectable formulation.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.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
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
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
Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors.Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.Proceedings of the National Academy of Sciences of the United States of America, , Jan-18, Volume: 97, Issue:2, 2000
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
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 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
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 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
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.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
2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 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
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 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],
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
[no title available],
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.European journal of medicinal chemistry, , Volume: 62, 2013
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.Proceedings of the National Academy of Sciences of the United States of America, , Jan-18, Volume: 97, Issue:2, 2000
[no title available],
An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.European journal of medicinal chemistry, , Jan-01, Volume: 209, 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
Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
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
Structural and functional basis of cyclooxygenase inhibition.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.Proceedings of the National Academy of Sciences of the United States of America, , Jan-18, Volume: 97, Issue:2, 2000
Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 2000
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Tuning the Dual Inhibition of Carbonic Anhydrase and Cyclooxygenase by Dihydrothiazole Benzensulfonamides.ACS medicinal chemistry letters, , Oct-11, Volume: 9, Issue:10, 2018
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase.Journal of medicinal chemistry, , May-26, Volume: 54, Issue:10, 2011
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
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],
Anti-inflammatory activity of triazine derivatives: A systematic review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
1,2-Diaryl-2-hydroxyiminoethanones as dual COX-1 and β-amyloid aggregation inhibitors: biological evaluation and in silico study.Chemical biology & drug design, , Volume: 85, Issue:4, 2015
Novel thiazolo[3,2-b]-1,2,4-triazoles derived from naproxen with analgesic/anti-inflammatory properties: Synthesis, biological evaluation and molecular modeling studies.Bioorganic & medicinal chemistry, , May-15, Volume: 23, Issue:10, 2015
Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
1-(4-Methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxamides: synthesis, molecular modeling, evaluation of their anti-inflammatory activity and ulcerogenicity.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
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
Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity.European journal of medicinal chemistry, , Volume: 57, 2012
Triterpene saponins from Clematis chinensis and their potential anti-inflammatory activity.Journal of natural products, , Jul-23, Volume: 73, Issue:7, 2010
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
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
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
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 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
Structure-based design of COX-2 selectivity into flurbiprofen.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Synthesis and anti-inflammatory activity of chalcone derivatives.Bioorganic & medicinal chemistry letters, , May-19, Volume: 8, 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
Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 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
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 22, Issue:13, 2012
Design, synthesis and biological evaluation of benzo[1.3.2]dithiazolium ylide 1,1-dioxide derivatives as potential dual cyclooxygenase-2/5-lipoxygenase inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 19, Issue:21, 2011
Bioactive sulfoximines: syntheses and properties of Vioxx analogs.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
A diazen-1-ium-1,2-diolated nitric oxide donor ester prodrug of 3-(4-hydroxymethylphenyl)-4-(4-methanesulfonylphenyl)-5H-furan-2-one: synthesis, biological evaluation and nitric oxide release studies.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
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 evaluation of dithiolethiones as novel cyclooxygenase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 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
Novel 2-(4-methylsulfonylphenyl)pyrimidine derivatives as highly potent and specific COX-2 inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.Journal of natural products, , Volume: 70, Issue:5, 2007
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
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 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
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
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
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
Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models.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
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
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 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
A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 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
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
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 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
Structure-Activity Relationships of Pentacyclic Triterpenoids as Inhibitors of Cyclooxygenase and Lipoxygenase Enzymes.Journal of natural products, , 12-27, Volume: 82, Issue:12, 2019
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 1998
Synthesis, inhibitory activity and in silico docking of dual COX/5-LOX inhibitors with quinone and resorcinol core.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
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
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
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammatory agents.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
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
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. 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
Structure-Activity Relationships of Pentacyclic Triterpenoids as Inhibitors of Cyclooxygenase and Lipoxygenase Enzymes.Journal of natural products, , 12-27, Volume: 82, Issue:12, 2019
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
Ursolic acid from Plantago major, a selective inhibitor of cyclooxygenase-2 catalyzed prostaglandin biosynthesis.Journal of natural products, , Volume: 61, Issue:10, 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
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
Synthesis of benzo-annulated tryptanthrins and their biological properties.Bioorganic & medicinal chemistry, , Aug-15, Volume: 20, Issue:16, 2012
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 26, Issue:6, 2016
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
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
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, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 2. 1,3,4- and 1,2,4-thiadiazole series.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
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
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
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
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
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
New celecoxib derivatives as anti-inflammatory agents.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
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
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
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
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
[no title available],
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.Journal of medicinal chemistry, , 08-12, Volume: 64, Issue:15, 2021
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Discovery of novel Methylsulfonyl phenyl derivatives as potent human Cyclooxygenase-2 inhibitors with effective anticonvulsant action: Design, synthesis, in-silico, in-vitro and in-vivo evaluation.European journal of medicinal chemistry, , May-10, Volume: 151, 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
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 Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents Journal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
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
Design, synthesis, and biological evaluation of some novel indolizine derivatives as dual cyclooxygenase and lipoxygenase inhibitor for anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-15, Volume: 25, Issue:16, 2017
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 22, Issue:15, 2012
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
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 26, Issue:6, 2016
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
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.The Journal of biological chemistry, , Jun-01, Volume: 282, Issue:22, 2007
[no title available]Journal of medicinal chemistry, , 09-22, Volume: 65, Issue:18, 2022
Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia.Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Lipid Peroxidation and Cyclooxygenase Enzyme Inhibitory Compounds from Prangos haussknechtii.Journal of natural products, , 09-22, Volume: 80, Issue:9, 2017
Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.Journal of medicinal chemistry, , 08-25, Volume: 59, Issue:16, 2016
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Ethanesulfohydroxamic acid ester prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs): synthesis, nitric oxide and nitroxyl release, cyclooxygenase inhibition, anti-inflammatory, and ulcerogenicity index studies.Journal of medicinal chemistry, , Mar-10, Volume: 54, Issue:5, 2011
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
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
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
[no title available],
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.ACS medicinal chemistry letters, , Oct-08, Volume: 6, Issue:10, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
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
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
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
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. 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
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
[no title available]Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo[d][1,3]dioxol-5-yl)-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents.Bioorganic chemistry, , Volume: 71, 2017
Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay.Journal of natural products, , Volume: 65, Issue:11, 2002
From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Anti-inflammatory and antioxidant properties of a novel resveratrol-salicylate hybrid analog.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 26, Issue:5, 2016
Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
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
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Constituents of the bark and twigs of Artocarpus dadah with cyclooxygenase inhibitory activity.Journal of natural products, , Volume: 65, Issue:2, 2002
N-Caffeoyl serotonin as selective COX-2 inhibitor.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 22, Issue:7, 2012
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.Journal of medicinal chemistry, , Mar-09, Volume: 49, Issue:5, 2006
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
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 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
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis, Inhibitory Activity, and ACS medicinal chemistry letters, , Apr-08, Volume: 12, Issue:4, 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
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
[no title available]Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Novel 1,3,4-oxadiazole/oxime hybrids: Synthesis, docking studies and investigation of anti-inflammatory, ulcerogenic liability and analgesic activities.Bioorganic chemistry, , Volume: 69, 2016
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
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]European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.European journal of medicinal chemistry, , Aug-15, Volume: 200, 2020
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.Bioorganic & medicinal chemistry, , 04-01, Volume: 28, Issue:7, 2020
Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.European journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Rational design, synthesis and evaluation of chromone-indole and chromone-pyrazole based conjugates: identification of a lead for anti-inflammatory drug.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Expanding the ChemGPS chemical space with natural products.Journal of natural products, , Volume: 68, Issue:7, 2005
Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.European journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
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 biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
[no title available],
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Acetohydroxamic acids as potent, selective, orally active 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
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
Medicinal chemistry of vicinal diaryl scaffold: A mini review.European journal of medicinal chemistry, , Jan-15, Volume: 162, 2019
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
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
Estimation of binding affinities for celecoxib analogues with COX-2 via Monte Carlo-extended linear response.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
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
Estimation of binding affinities for celecoxib analogues with COX-2 via Monte Carlo-extended linear response.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Three-dimensional quantitative structure-activity relationships of cyclo-oxygenase-2 (COX-2) inhibitors: a comparative molecular field analysis.Journal of medicinal chemistry, , Sep-27, Volume: 44, Issue:20, 2001
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
Antiinflammatory 4,5-diarylpyrroles. 2. Activity as a function of cyclooxygenase-2 inhibition.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
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 8 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] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| 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 8 target(s):
| Target | Category | Definition |
|---|
| nuclear inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the nuclear envelope. [GOC:ma] |
| nuclear outer membrane | cellular component | The outer, i.e. cytoplasm-facing, lipid bilayer of the nuclear envelope; continuous with the endoplasmic reticulum of the cell and sometimes studded with ribosomes. [ISBN:0198547684] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| endoplasmic reticulum lumen | cellular component | The volume enclosed by the membranes of the endoplasmic reticulum. [ISBN:0198547684] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| caveola | cellular component | A membrane raft that forms small pit, depression, or invagination that communicates with the outside of a cell and extends inward, indenting the cytoplasm and the cell membrane. Examples include flask-shaped invaginations of the plasma membrane in adipocytes associated with caveolin proteins, and minute pits or incuppings of the cell membrane formed during pinocytosis. Caveolae may be pinched off to form free vesicles within the cytoplasm. [GOC:mah, ISBN:0721662544, PMID:16645198] |
| 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/] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| 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/] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 59 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] |
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| 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] |
| embryo implantation | biological process | Attachment of the blastocyst to the uterine lining. [GOC:isa_complete, http://www.medterms.com] |
| learning | biological process | Any process in an organism in which a relatively long-lasting adaptive behavioral change occurs as the result of experience. [ISBN:0582227089, ISBN:0721662544] |
| memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
| 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] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| response to xenobiotic stimulus | 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 a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| response to nematode | 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 a stimulus from a nematode. [GOC:hb] |
| response to fructose | 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 a fructose stimulus. [GOC:jl] |
| response to manganese ion | 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 a manganese ion stimulus. [GOC:sm] |
| positive regulation of vascular endothelial growth factor production | biological process | Any process that increases or activates the frequency, rate, or extent of production of vascular endothelial growth factor. [GOC:BHF, GOC:rl] |
| 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] |
| bone mineralization | biological process | The deposition of hydroxyapatite, a form of calcium phosphate with the formula Ca10(PO4)6(OH)2, in bone tissue. [GOC:mah, PMID:22936354] |
| positive regulation of prostaglandin biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of prostaglandin. [GOC:mah] |
| positive regulation of fever generation | biological process | Any process that activates or increases the frequency, rate, or extent of fever generation. [GOC:add] |
| positive regulation of synaptic plasticity | biological process | A process that increases synaptic plasticity, the ability of synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:mah] |
| negative regulation of synaptic transmission, dopaminergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of dopaminergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter dopamine. [GOC:mah] |
| prostaglandin secretion | biological process | The regulated release of a prostaglandin, any of a group of biologically active metabolites which contain a cyclopentane ring, from a cell or a tissue. [GOC:mah] |
| response to estradiol | 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| positive regulation of peptidyl-serine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-serine. [GOC:mah] |
| response to vitamin D | 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 a vitamin D stimulus. [GOC:sl] |
| cellular response to heat | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a heat stimulus, a temperature stimulus above the optimal temperature for that organism. [GOC:mah] |
| response to tumor necrosis factor | 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 a tumor necrosis factor stimulus. [GOC:mah] |
| maintenance of blood-brain barrier | biological process | Maintaining the structure and function of the blood-brain barrier, thus ensuring specific regulated transport of substances (e.g. macromolecules, small molecules, ions) into the brain, and out of the brain into the blood circulation. [GOC:aruk, GOC:bc, GOC:bf, GOC:sl, PMID:20080302, PMID:30280653] |
| positive regulation of protein import into nucleus | biological process | Any process that activates or increases the frequency, rate or extent of movement of proteins from the cytoplasm into the nucleus. [GOC:jl] |
| hair cycle | biological process | The cyclical phases of growth (anagen), regression (catagen), quiescence (telogen), and shedding (exogen) in the life of a hair; one of the collection or mass of filaments growing from the skin of an animal, and forming a covering for a part of the head or for any part or the whole of the body. [GOC:go_curators, PMID:12230507] |
| positive regulation of apoptotic process | biological process | Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of nitric oxide biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of nitric oxide. [GOC:go_curators] |
| negative regulation of cell cycle | biological process | Any process that stops, prevents or reduces the rate or extent of progression through the cell cycle. [GOC:dph, GOC:go_curators, GOC:tb] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| negative regulation of smooth muscle contraction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| positive regulation of smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| decidualization | biological process | The cellular and vascular changes occurring in the endometrium of the pregnant uterus just after the onset of blastocyst implantation. This process involves the proliferation and differentiation of the fibroblast-like endometrial stromal cells into large, polyploid decidual cells that eventually form the maternal component of the placenta. [ISBN:0721662544, PMID:11133685] |
| positive regulation of smooth muscle cell proliferation | biological process | Any process that activates or increases the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| regulation of inflammatory response | biological process | Any process that modulates the frequency, rate or extent of the inflammatory response, the immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. [GOC:ai] |
| brown fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a brown adipocyte, an animal connective tissue cell involved in adaptive thermogenesis. Brown adipocytes contain multiple small droplets of triglycerides and a high number of mitochondria. [PMID:12588810] |
| response to glucocorticoid | 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 a glucocorticoid stimulus. Glucocorticoids are hormonal C21 corticosteroids synthesized from cholesterol with the ability to bind with the cortisol receptor and trigger similar effects. Glucocorticoids act primarily on carbohydrate and protein metabolism, and have anti-inflammatory effects. [GOC:ai, PMID:9884123] |
| negative regulation of calcium ion transport | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| positive regulation of synaptic transmission, glutamatergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
| response to fatty acid | 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 a fatty acid stimulus. [GOC:lp] |
| cellular response to mechanical stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mechanical stimulus. [GOC:mah] |
| cellular response to lead ion | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lead ion stimulus. [GOC:mah] |
| cellular response to ATP | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ATP (adenosine 5'-triphosphate) stimulus. [GOC:mah] |
| cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| cellular response to non-ionic osmotic stress | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating an increase or decrease in the concentration of non-ionic solutes (e.g. mannitol, sorbitol) in the environment. [GOC:mah] |
| cellular response to fluid shear stress | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a fluid shear stress stimulus. Fluid shear stress is the force acting on an object in a system where the fluid is moving across a solid surface. [GOC:mah] |
| positive regulation of transforming growth factor beta production | biological process | Any process that activates or increases the frequency, rate, or extent of production of transforming growth factor-beta. [GOC:mah] |
| positive regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that increases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
| positive regulation of fibroblast growth factor production | biological process | Any process that increases the rate, frequency or extent of the appearance of a fibroblast growth factor due to biosynthesis or secretion following a cellular stimulus, resulting in an increase in its intracellular or extracellular levels. [GOC:BHF] |
| positive regulation of brown fat cell differentiation | biological process | Any process that increases the rate, frequency, or extent of brown fat cell differentiation. Brown fat cell differentiation is the process in which a relatively unspecialized cell acquires specialized features of a brown adipocyte, an animal connective tissue cell involved in adaptive thermogenesis. Brown adipocytes contain multiple small droplets of triglycerides and a high number of mitochondria. [GOC:BHF] |
| positive regulation of platelet-derived growth factor production | biological process | Any process that increases the rate, frequency, or extent of the appearance of any platelet-derived growth factor due to biosynthesis or secretion following a cellular stimulus, resulting in an increase in its intracellular or extracellular levels. [GOC:BHF] |
| 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] |
| regulation of neuroinflammatory response | biological process | Any process that modulates the frequency, rate or extent of neuroinflammatory response. [GOC:aruk, GOC:bc, PMID:10981966, PMID:11099416, PMID:18164423] |
| negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of intrinsic apoptotic signaling pathway in response to osmotic stress. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl, GOC:TermGenie, PMID:14569084] |
| cellular response to homocysteine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a homocysteine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:26722473] |
| response to angiotensin | 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 an angiotensin stimulus. Angiotensin is any of three physiologically active peptides (angiotensin II, III, or IV) processed from angiotensinogen. [PMID:22982863] |