681247-97-2Relevant academic research and scientific papers
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids
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.
, p. 2817 - 2822 (2008/02/03)
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
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Page 111, (2008/06/13)
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.
Sulfonamides having antiangiogenic and anticancer activity
-
, (2008/06/13)
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.
