Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups.
The structure-based design of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1' groups has led to compounds with excellent in vitro potency against TACE and selectivity over MMP-1.
Chen
James M
JM
Wyeth-Ayerst Research, 401N. Middletown Road, Pearl River, NY 10965, USA. jchen@gilead.com
Jin
Guixian
G
Sung
Amy
A
Levin
Jeremy I
JI
D051722:ADAM Proteins; D000072198:ADAM17 Protein; D000114:Acetylene / Q000737:chemistry*; D000595:Amino Acid Sequence; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006877:Hydroxamic Acids / Q000737:chemistry* / Q000494:pharmacology*; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D008969:Molecular Sequence Data; D015394:Molecular Structure; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D062367:ortho-Aminobenzoates / Q000737:chemistry* / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D013449:Sulfonamides; D062367:ortho-Aminobenzoates; D051722:ADAM Proteins; D008666:Metalloendopeptidases; D000072198:ADAM17 Protein; D000114:Acetylene