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Review

Inhibitors of cyclooxygenase-2: November 1999 - April 2000

Pages 1011-1020 | Published online: 25 Feb 2005

Bibliography

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  • •This paper provides data on the lack of selectivity of current NSAIDs as well as selectivity data on new selective COX-2 series.
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  • ••This paper provides key basic research data in support ofuse of selective COX-2 to provide the positive effects of pain and inflammation relief associated with non-selective COX inhibitors.
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  • ••This paper provides evidence that selective COX-2 inhibi-tors are anti-inflammatory without displaying the GI side effect profile common to all NSAIDs.
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  • ••This previous review provides an excellent resource to theearlier patent literature.
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  • •This discovery of NS-398 as a selective COX-2 inhibitor is one of the landmark events in the development of selective COX-2 inhibitors. The work presented led to the discovery of many similar selective COX-2 agents.
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  • •This paper describes the optimisation approach used by Merck Frosst to develop one of the series of selective COX-2 inhibitors.
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  • ••This paper describes the impressive safety and efficacyprofile of DuP 697, which was to become probably the most important lead in the search for a selective COX-2 inhibitor.
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  • •This paper provides detailed SAR and early PK data leading to the discovery and development of celecoxib, one of the selective COX-2 inhibitors currently in clinical trials.
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  • ••This paper provides a definitive study of the nature ofselective inhibition of COX-2 by 'DFU' and its slow reversi-bility. In addition, this paper discloses some of the variation in assay conditions which provide different COX selectivity.
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  • •This paper describes the conversion of one of the most efficaceous NSAIDs into a selective COX-2 inhibitor.
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  • ••This paper provides kinetic data on the nature of selectiveCOX-2 inhibition and its slow reversibility.
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  • ••This paper provides the earliest reported data explaining thenature of 'irreversible' inhibition of COX-2.
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  • •This review details the theory and data supporting the study of COX-2 inhibitors in oncology.
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  • •This review details the theory and data supporting the study of COX-2 inhibitors in oncology.
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  • •This review details the theory and data supporting the study of COX-2 inhibitors in treatment of neurodegenerative diseases.

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