Synthesis of a novel family of diterpenes and their evaluation as anti-inflammatory agents.
The synthesis and biological evaluation of a new family of diterpenes, represented by structures 2 and 3, is presented. These compounds constitute isomeric analogues of acanthoic acid (1) and were examined as potent anti-inflammatory agents. Among them, methyl ester 12 exhibited a low non-specific cytotoxicity, inhibited TNF-alpha synthesis and displayed good specificity in suppressing cytokine expression.
Lam
Thanh
T
Department of Chemistry and Biochemistry, University of California-San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0358, USA.
Ling
Taotao
T
Chowdhury
Chinmay
C
Chao
Ta-Hsiang
TH
Bahjat
F R
FR
Lloyd
G K
GK
Moldawer
Lyle L
LL
Palladino
Michael A
MA
Theodorakis
Emmanuel A
EA
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004224:Diterpenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D028001:Eleutherococcus; D006801:Humans; D010936:Plant Extracts / Q000138:chemical synthesis / Q000494:pharmacology; D018517:Plant Roots; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004224:Diterpenes; D010936:Plant Extracts; D014409:Tumor Necrosis Factor-alpha