Synthesis and SAR of highly selective MMP-13 inhibitors.
The structure-based design and synthesis of a series of novel biphenyl sulfonamide carboxylic acids as potent MMP-13 inhibitors with selectivity over MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-14, Aggrecanase 1, and TACE are described.
Li
Jianchang
J
Department of Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. JCLI@wyeth.com
Rush
Thomas S
TS
Li
Wei
W
DeVincentis
Dianne
D
Du
Xuemei
X
Hu
Yonghan
Y
Thomason
Jennifer R
JR
Xiang
Jason S
JS
Skotnicki
Jerauld S
JS
Tam
Steve
S
Cunningham
Kristina M
KM
Chockalingam
Priya S
PS
Morris
Elisabeth A
EA
Levin
Jeremy I
JI
D000586:Amination; D001572:Benzofurans / Q000737:chemistry; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017364:Collagenases / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D053509:Matrix Metalloproteinase 13; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry
D001572:Benzofurans; D002264:Carboxylic Acids; D004791:Enzyme Inhibitors; D061965:Matrix Metalloproteinase Inhibitors; D013455:Sulfur; D017364:Collagenases; D053509:Matrix Metalloproteinase 13