Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377244 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn2+ as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.
Graphical abstractSynthesis and biological activity of novel methionine aminopeptidase type -2 inhibitors having a sulfonamide bond are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Megumi Kawai, Nwe Y. BaMaung, Steve D. Fidanze, Scott A. Erickson, Jason S. Tedrow, William J. Sanders, Anil Vasudevan, Chang Park, Charles Hutchins, Kenneth M. Comess, Douglas Kalvin, Jieyi Wang, Qian Zhang, Pingping Lou, Lora Tucker-Garcia,