Lead discovery of alpha,beta-unsaturated sulfones from a combinatorial library as inhibitors of inducible VCAM-1 expression.
alpha,beta-Unsaturated sulfones have been discovered from a combinatorial library as leads for a new series of inhibitors of inducible VCAM-1 expression. Although not essential, further conjugation of the sulfonyl group to another vinyl group or a phenyl group increases the potency dramatically.
Ni
Liming
L
AtheroGenics, Inc., 8995 Westside Parkway, Alpharetta, GA 30004, USA.
Zheng
X Sharon
XS
Somers
Patricia K
PK
Hoong
Lee K
LK
Hill
Russell R
RR
Marino
Elaine M
EM
Suen
Ki-Ling
KL
Saxena
Uday
U
Meng
Charles Q
CQ
D002478:Cells, Cultured; D020650:Combinatorial Chemistry Techniques; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry* / Q000494:pharmacology*; D019010:Vascular Cell Adhesion Molecule-1 / Q000096:biosynthesis / Q000187:drug effects*
D013450:Sulfones; D019010:Vascular Cell Adhesion Molecule-1