Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
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Pal M, Rao Veeramaneni V, Nagabelli M, Rao Kalleda S, Misra P, Rao Casturi S, Rao Yeleswarapu K
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett. 2003 May 19;13(10):1639-43.
- PubMed ID
- 12729631 [ View in PubMed]
- Abstract
A number of naphthofuranones were synthesized and tested for COX-1 and COX-2 inhibition. Few of them were identified as selective COX-2 inhibitors. Structure-activity relationship studies within the series are discussed.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 36 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 329 N/A N/A Details