Abstract
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.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Hydroxamic Acids / chemical synthesis
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Hydroxamic Acids / chemistry*
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Hydroxamic Acids / pharmacology*
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Indoles / chemistry
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Indoles / pharmacology
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Inhibitory Concentration 50
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Matrix Metalloproteinase Inhibitors*
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacology*
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Recombinant Proteins / antagonists & inhibitors
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Structure-Activity Relationship
Substances
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Hydroxamic Acids
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Indoles
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Matrix Metalloproteinase Inhibitors
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Protease Inhibitors
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Recombinant Proteins
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ilomastat