Journal ArticleDOI
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors.
M. V. Ramana Reddy,Vinay K. Billa,Venkat R. Pallela,Muralidhar R. Mallireddigari,Rengasamy Boominathan,Jerome L. Gabriel,E. Premkumar Reddy +6 more
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TLDR
Molecular modeling and comparison of molecular models of 5a enantiomers with that of celecoxib model shows that 5a (enantiomer-1) and 5a-2 have more hydrogen bonding interactions in the catalytic domain of COX-2 enzyme than cele Coxib.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2008-04-01. It has received 104 citations till now. The article focuses on the topics: Cyclooxygenase & Pyrazoline.read more
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Evolution of nonsteroidal anti-inflammatory drugs (NSAIDs): cyclooxygenase (COX) inhibition and beyond
P.N. Praveen Rao,Edward E. Knaus +1 more
TL;DR: This review traces the origins of NSAIDs, their mechanism of action at the molecular level such as cyclooxygenase (COX) inhibition, development of selective COX-2 inhibitors, their adverse cardiovascular effects, and some recent developments targeted to the design of effective anti-inflammatory agents with reduced side effects.
Journal ArticleDOI
Synthesis of novel pyrazolic analogues of chalcones and their 3-aryl-4-(3-aryl-4,5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazole derivatives as potential antitumor agents
Braulio Insuasty,Alexis Tigreros,Fabian Orozco,Jairo Quiroga,Rodrigo Abonia,Manuel Nogueras,Adolfo Sánchez,Justo Cobo +7 more
TL;DR: Several novel compounds synthesized from a Claisen-Schmidt reaction of 3-aryl-1-phenylpyrazol-4-carboxaldehydes 4 with several acetophenone derivatives were screened by the US National Cancer Institute for their ability to inhibit 60 different human tumor cell lines.
Journal ArticleDOI
Photocatalytic Radical Trifluoromethylation/Cyclization Cascade: Synthesis of CF3-Containing Pyrazolines and Isoxazolines.
TL;DR: A general visible light induced photoredox-catalyzed radical trifluoromethylation/cyclization cascade of β-aryl-β,γ-unsaturated hydrazones and oximes is described.
Journal ArticleDOI
Biological activities of pyrazoline derivatives--a recent development.
TL;DR: The present review provides an insight view to pyrazolines synthesis and its biological activities along with the compilation of recent patents on pyrazoline derivatives.
Journal ArticleDOI
Synthesis and bioactivity studies on new 4-(3-(4-Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2-c]pyrazol-2-yl) benzenesulfonamides.
Halise Inci Gul,Mehtap Tugrak,Hiroshi Sakagami,Parham Taslimi,İlhami Gülçin,Claudiu T. Supuran +5 more
TL;DR: The 3,4,5-trimethoxy and the 4-hydroxy derivatives showed interesting cytotoxic activities, which may be crucial for further anti-tumor activity studies, whereas some of these sulfonamides strongly inhibited both human (h) cytosolic isoforms hCA I and II.
References
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Journal ArticleDOI
Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs
TL;DR: Experiments with guinea-pig lung suggest that some of the therapeutic effects of sodium salicylate and aspirin-like drugs are due to inhibition of the synthesis of prostaglandins.
Journal ArticleDOI
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).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more
TL;DR: 1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis, is identified.
Journal ArticleDOI
Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents.
Ravi G. Kurumbail,Anna M. Stevens,James K. Gierse,Joseph J. McDonald,Roderick A. Stegeman,Jina Y. Pak,Daniel Gildehaus,Julie M. Miyashiro,Thomas D. Penning,Karen Seibert,Peter C. Isakson,William C. Stallings +11 more
TL;DR: The structures of unliganded murine COX-2 and complexes with flurbiprofen, indomethacin and SC-558, a selective COx-2 inhibitor, determined are explained and some of the conformational changes associated with time-dependent inhibition are demonstrated.
Journal ArticleDOI
Aspirin selectively inhibits prostaglandin production in human platelets
TL;DR: Platelets in the blood of volunteers who have taken aspirin can no longer produce prostaglandins, and these platelets are removed from the body by the immune system.
Journal ArticleDOI
Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs.
TL;DR: Results demonstrate that the two PGH synthases are pharmacologically distinct and indicate that it may be possible to develop isozyme-specific cyclooxygenase inhibitors useful both for anti-inflammatory therapy and for delineating between the biological roles of the P GH synthase isozymes.
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Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) as a new strategy to provide safer non-steroidal anti-inflammatory drugs
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).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more