Thalidomide analogs and PDE4 inhibition

G W Muller; M G Shire; L M Wong; L G Corral; R T Patterson; Y Chen; D I Stirling

doi:10.1016/s0960-894x(98)00475-2

Thalidomide analogs and PDE4 inhibition

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74. doi: 10.1016/s0960-894x(98)00475-2.

Authors

G W Muller¹, M G Shire, L M Wong, L G Corral, R T Patterson, Y Chen, D I Stirling

Affiliation

¹ Celgene Corporation, Warren, NJ 07059 USA.

PMID: 9873600
DOI: 10.1016/s0960-894x(98)00475-2

Abstract

N-Phthaloyl 3-amino-3-arylpropionic acid analogs of thalidomide that are potent inhibitors of tumor necrosis factor-alpha are reported. These compounds were found to be potent inhibitors of phosphodiesterase 4.

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
Cyclic Nucleotide Phosphodiesterases, Type 4
Humans
Leukocytes, Mononuclear / drug effects
Leukocytes, Mononuclear / metabolism
Lipopolysaccharides / pharmacology
Phosphodiesterase Inhibitors / chemistry
Phosphodiesterase Inhibitors / pharmacology*
Structure-Activity Relationship
Thalidomide / analogs & derivatives*
Thalidomide / chemistry
Thalidomide / pharmacology
Tumor Cells, Cultured
Tumor Necrosis Factor-alpha / antagonists & inhibitors

Substances

Lipopolysaccharides
Phosphodiesterase Inhibitors
Tumor Necrosis Factor-alpha
Thalidomide
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 4