Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids

A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2). Small alkyl groups and 3-furyl were tolerated at the 5-position of anthranilic acid, while –OCH 3, CH 3, and Cl were found optimal for the 6-position. Pl...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (10), p.2817-2822
Hauptverfasser:	Wang, Gary T., Mantei, Robert A., Kawai, Megumi, Tedrow, Jason S., Barnes, David M., Wang, Jieyi, Zhang, Qian, Lou, Pingping, Garcia, Lora A., Bouska, Jennifer, Yates, Melinda, Park, Chang, Judge, Russell A., Lesniewski, Richard, Sheppard, George S., Bell, Randy L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopeptidases - antagonists & inhibitors Aminopeptidases - chemistry Antineoplastic agents Biological and medical sciences General aspects Lead - chemistry Medical sciences Metalloendopeptidases - antagonists & inhibitors Metalloendopeptidases - chemistry Methionine aminopeptidase-2 (MetAP2) inhibitors Models, Molecular Molecular Structure ortho-Aminobenzoates - chemistry ortho-Aminobenzoates - pharmacology Pharmacology. Drug treatments Protein Conformation Structure-Activity Relationship Sulfonamides - chemistry Sulfonamides of 5,6-disubstituted anthranilic acids
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