Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the Ugi four-component condensation
A library of 108 α,α-difluoromethylenephosphonic acids was prepared by Ugi four-component condensation using Rink-NH2 resin, 4- [(diethoxyphosphinyl)difluoromethyl]benzoic acid, and a set of 18 aldehydes and 6 isonitriles. Following resin cleavage, the diethylphosphonate esters were hydrolyzed with trimethylsilyl bromide to yield the free acids which were assayed for inhibition of PTPα, PTPβ and PTPε.
Li, Zhengong,Yeo, Su Ling,Pallen, Catherine J.,Ganesan
Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction
The eukaryotic initiation factor 4E (eIF4E) plays a central role in the initiation of gene translation and subsequent protein synthesis by binding the 5′ terminal mRNA cap structure. We designed and synthesized a series of novel compounds that display pot
Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA
The development of low μM inhibitors of the Mycobacterium tuberculosis phosphatase PtpA is reported. The most potent of these inhibitors (Ki = 1.4 ± 0.3 μM) was found to be selective when tested against a panel of human tyrosine and dual-specif
Rawls, Katherine A.,Therese Lang,Takeuchi, Jun,Imamura, Shinichi,Baguley, Tyler D.,Grundner, Christoph,Alber, Tom,Ellman, Jonathan A.
supporting information; experimental part
p. 6851 - 6854
(2010/06/16)
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