Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents

R Gautam, SM Jachak, V Kumar, CG Mohan

Index: Gautam, Raju; Jachak, Sanjay M.; Kumar, Vivek; Mohan, C. Gopi Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1612 - 1616

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Citation Number: 21

Abstract

Stellatin (4), isolated from Dysophylla stellata is a cyclooxygenase (COX) inhibitor. The present study reports the synthesis and biological evaluation of new stellatin derivatives for COX-1, COX-2 inhibitory and anti-inflammatory activities. Eight derivatives showed more pronounced COX-2 inhibition than stellatin and, 17 and 21 exhibited the highest COX-2 inhibition. They also exhibited the significant anti-inflammatory activity in TPA-induced ...