Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis.
A series of novel phenolic compounds has been discovered as potent inhibitors of TNF-alpha-inducible expression of vascular cell adhesion molecule-1 (VCAM-1) with concurrent antioxidant and lipid-modulating properties. Optimization of these multifunctional agents led to the identification of 3a (AGI-1067) as a clinical candidate with demonstrated efficacies in animal models of atherosclerosis and hyperlipidemia.
AtheroGenics, Inc., 8995 Westside Parkway, GA 30004, Alpharetta, USA. cmeng@atherogenics.com
Charles Q
CQ
Meng
Patricia K
PK
Somers
Carolyn L
CL
Rachita
Lisa A
LA
Holt
Lee K
LK
Hoong
X Sharon
XS
Zheng
Jacob E
JE
Simpson
Russell R
RR
Hill
Lynda K
LK
Olliff
Charles
C
Kunsch
Cynthia L
CL
Sundell
Sampath
S
Parthasarathy
Uday
U
Saxena
James A
JA
Sikorski
Martin A
MA
Wasserman
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology* / Q000627:therapeutic use; D001161:Arteriosclerosis / Q000188:drug therapy / Q000378:metabolism*; D006801:Humans; D010636:Phenols / Q000494:pharmacology* / Q000627:therapeutic use; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors; D019010:Vascular Cell Adhesion Molecule-1 / Q000378:metabolism*
D000975:Antioxidants; D010636:Phenols; D014409:Tumor Necrosis Factor-alpha; D019010:Vascular Cell Adhesion Molecule-1