215734-82-0Relevant articles and documents
Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the Ugi four-component condensation
Li, Zhengong,Yeo, Su Ling,Pallen, Catherine J.,Ganesan
, p. 2443 - 2446 (1998)
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.
Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction
Chen, Xiaoqi,Kopecky, David J.,Mihalic, Jeff,Jeffries, Shawn,Min, Xiaoshan,Heath, Julie,Deignan, Jeff,Lai, Sujen,Fu, Zice,Guimaraes, Cristiano,Shen, Shanling,Li, Shyun,Johnstone, Sheree,Thibault, Stephen,Xu, Haoda,Cardozo, Mario,Shen, Wang,Walker, Nigel,Kayser, Frank,Wang, Zhulun
experimental part, p. 3837 - 3851 (2012/07/28)
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
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)
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
