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Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids by Gary T. Wang; Robert A. Mantei; Megumi Kawai; Jason S. Tedrow; David M. Barnes; Jieyi Wang; Qian Zhang; Pingping Lou; Lora A. Garcia; Jennifer Bouska; Melinda Yates; Chang Park; Russell A. Judge; Richard Lesniewski; George S. Sheppard; Randy L. Bell is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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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. Placement of 2-aminoethoxy group at the 6-position enabled interaction with the second Mn 2+ 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.

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Author

Gary T. Wang; Robert A. Mantei; Megumi Kawai; Jason S. Tedrow; David M. Barnes; Jieyi Wang; Qian Zhang; Pingping Lou; Lora A. Garcia; Jennifer Bouska; Melinda Yates; Chang Park; Russell A. Judge; Richard Lesniewski; George S. Sheppard; Randy L. Bell

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2007

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)