681247-98-3

Upstream product

• 681247-97-2 methyl 6-amino-2-methoxy-3-vinylbenzoate 
• 67765-42-8 5-methoxy-2,4-dihydro-1H-3,1-benzoxazine-2,4-dione 
• 53600-33-2 6-methoxyanthranilic acid 
• 681247-48-3 methyl 6-amino-3-bromo-2-methoxybenzoate 
• 681247-09-6 6-bromo-5-methoxy-2,4-dihydro-1H-3,1-benzoxazine-2,4-dione 

Relevant academic research and scientific papers

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 -OCH3, CH3, and Cl were found optimal for the 6-position. Placement of 2-aminoethoxy group at the 6-position enabled interaction with the second Mn2+ but did not result in enhancement in potency. Introduction of a tertiary amino moiety at the ortho-position of the sulfonyl phenyl ring gave reduced protein binding and improved cellular activity, but led to lower oral bioavailability.

Sulfonamides having antiangiogenic and anticancer activity

Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.