Synthesis and TNF expression inhibitory properties of new thalidomide analogues derived via Heck cross coupling.
A library of new thalidomide analogues containing an olefin functionality were synthesised using a Heck cross coupling reaction from their aryl halogenated precursor. All analogues were tested for their ability to inhibit the synthesis of the proinflammatory cytokine Tumour Necrosis Factor (TNF). Compounds 22, 29, 33 and 37 were the most effective in this assay inhibiting TNF expression 50%, 69%, 52% and 50%, respectively.
Stewart
Scott G
SG
The School of Biomedical, Biomolecular & Chemical Sciences, The University of Western Australia, Crawley, WA 6009, Australia. sgs@cyllene.uwa.edu.au
Spagnolo
Daniel
D
Polomska
Marta E
ME
Sin
Melvin
M
Karimi
Mahdad
M
Abraham
Lawrence J
LJ
D006801:Humans; D019169:Jurkat Cells; D013792:Thalidomide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis* / Q000378:metabolism
D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide