4559-92-6Relevant articles and documents
Broad Scope and High-Yield Access to Unsymmetrical Acyclic [11C]Ureas for Biomedical Imaging from [11C]Carbonyl Difluoride
Jakobsson, Jimmy E.,Jana, Susovan,Lu, Shuiyu,Pike, Victor W.,Telu, Sanjay
supporting information, p. 10369 - 10376 (2021/06/07)
Effective methods are needed for labelling acyclic ureas with carbon-11 (t1/2=20.4 min) as potential radiotracers for biomedical imaging with positron emission tomography (PET). Herein, we describe the rapid and high-yield syntheses of unsymmet
Structure–activity relationships (SARs) of α- ketothioamides as inhibitors of phosphoglycerate dehydrogenase (PHGDH)
Spillier, Quentin,Ravez, Séverine,Unterlass, Judith,Corbet, Cyril,Degavre, Charline,Feron, Olivier,Frédérick, Rapha?l
, (2020/02/11)
For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the serine synthetic pathway, and particularly of the phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the pathway, to sustain cancer progression. Yet, because of very weak potencies usually in cell-based settings, the inhibitors reported so far failed to lay ground on the potential of this approach. In this paper, we report a structure–activity relationship study of a series of α-ketothioamides that we have recently identified. Interestingly, this study led to a deeper understanding of the structure–activity relationship (SAR) in this series and to the identification of new PHGDH inhibitors. The activity of the more potent compounds was confirmed by cellular thermal shift assays and in cell-based experiments. We hope that this research will eventually provide a new entry point, based on this promising chemical scaffold, for the development of therapeutic agents targeting PHGDH.
Method for preparing asymmetric urea compound (by machine translation)
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Paragraph 0043-0048, (2020/03/25)
The invention provides a vehicle CO. 2 A method. for synthesizing an asymmetric urea compound by carbonylation coupling reaction of the carbonylation reagent is: and the aromatic, aliphatic primary amine compound and the aliphatic secondary amine compound and the normal pressure (100 °C, diglyme), can be efficiently prepared by using a common Lewis base and a hydrogen silane as the accelerator/CO under mild conditions. 2 The reaction produces a corresponding asymmetric urea compound. containing different functional groups, the process being operated at atmospheric pressure CO. 2 The use of an inexpensive Lewis base and, industrial silicon waste PMHS( for the green non-toxic carbonylation reagent) avoids toxic carbonylation reagents, high pressure, as an accelerator CO. 2 , The use, of the expensive dehydrating agent and the noble metal does not need to purify and separate the intermediate, and the pure product, is obtained by simple suction filtration separation after the reaction is ended . is a high efficiency, novel synthetic method . The commercial herbicide NEBURON. is successfully prepared by using the method. (by machine translation)
