Synthesis of new ent-labdane diterpene derivatives from andrographolide and evaluation of their anti-inflammatory activities
Abstract
Two series of andrographolide derivatives with nitrogen-containing heterocycles, phenols and aromatic acids as bioisostere moiety of lactone ring were synthesized. 8 from 18 tested compounds showed stronger inhibitory effect on LPS-induced NO production in RAW264.7 macrophage than hydrocortisone. Among them, compound 8m exhibited the most potent inhibition with IC50 of 3.38 ± 1.03 μM. The structure-activity relationships (SARs) suggested that...
Paper Details
Title
Synthesis of new ent-labdane diterpene derivatives from andrographolide and evaluation of their anti-inflammatory activities
Published Date
Jan 1, 2019
Volume
162
Pages
70 - 79
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