Design, Synthesis and Evaluation of AdSS Bisubstrate Inhibitors
Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and evaluated against purified AdSS. The best activity was obtained with adenosine bearing a four-carbon linker that connects the N-formyl-N-hydroxy moiety to the 6-position of the purine nucleoside.
Tibrewal, Nidhi,Elliott, Gregory I.
supporting information
p. 2269 - 2272
(2020/09/17)
ANTIBACTERIAL SIDEROMYCINS
A compound, comprising: an Fe(III)-binding and/or Fe(III)-bound siderophore; one or more optional linker covalently bound to the siderophore; and daptomycin covalently bound to the linker, or, if no linker is present, then to the siderophore; or pharmaceu
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Page/Page column 82
(2016/03/13)
PYRIMIDINONE COMPOUNDS AND METHODS FOR PREVENTING AND TREATING INFLUENZA
In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching
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Page/Page column 64
(2012/11/14)
The preparation of a fully differentiated "multiwarhead" siderophore precursor
A protected, fully differentiated siderophore analogue has been prepared so that "Trojan Horse"-like siderophore drug conjugates with different drugs can be synthesized. The key steps in the synthesis include controlled preparation of an unsymmetrical urea and its conversion to a fully differentiated isocyanurate by reaction with chloro(carbonyl) isocyanate.
Murray, Aaron P.,Miller, Marvin J.
p. 191 - 194
(2007/10/03)
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