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Bioorg Med Chem. 2009 Feb 1;17(3):1044-54. doi: 10.1016/j.bmc.2008.04.031. Epub 2008 May 16.

Synthesis and biological evaluation of a library of resveratrol analogues as inhibitors of COX-1, COX-2 and NF-kappaB.

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Department of Chemistry, The Purdue Cancer Center, Purdue University, 560 Oval Drive, West Lafayette, IN 47907-2084, USA.


Resveratrol (4,3',5'-trihydroxystilbene) is a naturally occurring antioxidant that inhibits cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) and the transcription factor NF-kappaB. A 78-membered library of resveratrol analogues in which the substituents on the two aryl rings and alkene were varied was synthesized using a solid-phase Wittig olefination reaction. The library contains inhibitors against all three proteins that were more potent than resveratrol itself. Preliminary structure-activity relationships were also obtained from these data that permitted the derivation of pharmacophore models for each of the three targets.

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