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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 26, Number 12
BKCSDE 26(12)
December 20, 2005 

 
Title
Synthesis and COX Inhibitory Activities of Rutaecarpine Derivatives
Author
Eung Seok Lee*, Seung Ill Kim, Seung Hoo Lee, Tae Cheon Jeong, Tae Chul Moon, Hyeun Wook Chang, Yurngdong Jahng*
Keywords
Rutaecarpine, COX-2 inhibitor, Antiinflammatory activity, Indoloquinazoline alkaloid
Abstract
A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity (IC50 = 0.27, 0.35 μM, respectively) with selectivity.
Page
1975 - 0
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