MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3.
Some ilomastat analogues featuring an isobutylidene group or a 2-substituted indole nucleus were synthesized to evaluate their inhibitory activities against gelatinase A and stromelysin-1. Potent MMP-2 inhibition and good selectivity for that enzyme have been observed for compounds 1a, 2 and 22.
Marcq
Valérie
V
IFR 53, UMR/CNRS 6013, Faculté de Pharmacie, 51 rue Cognacq-Jay, 51096 Reims Cedex, France.
Mirand
Catherine
C
Decarme
Martine
M
Emonard
Hervé
H
Hornebeck
William
W
D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D006877:Hydroxamic Acids; D007211:Indoles; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D011994:Recombinant Proteins; C119203:ilomastat