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.
Meng
Charles Q
CQ
AtheroGenics, Inc., 8995 Westside Parkway, GA 30004, Alpharetta, USA. cmeng@atherogenics.com
Somers
Patricia K
PK
Rachita
Carolyn L
CL
Holt
Lisa A
LA
Hoong
Lee K
LK
Zheng
X Sharon
XS
Simpson
Jacob E
JE
Hill
Russell R
RR
Olliff
Lynda K
LK
Kunsch
Charles
C
Sundell
Cynthia L
CL
Parthasarathy
Sampath
S
Saxena
Uday
U
Sikorski
James A
JA
Wasserman
Martin A
MA
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