351186-42-0Relevant articles and documents
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.
The Design of an In-Ex Tube for Gas Related Organic Reactions
Yin, Zhiping,Wu, Xiao-Feng
, p. 1869 - 1871 (2017/11/24)
Here, an interesting in-ex tube was designed for gas-related organic reactions. By using this specially designed reaction tube, several gas-reliant organic reactions are applicable, including CO, SO2, and H2. Moderate to good yields of the desired products were produced easily.
A copper-catalyzed three-component reaction of triethoxysilanes, sulfur dioxide, and hydrazines
Wang, Xianbo,Xue, Lijun,Wang, Zhiyong
supporting information, p. 4056 - 4058 (2014/08/18)
A three-component reaction of triethoxysilanes, sulfur dioxide, and hydrazines catalyzed by copper(II) acetate is reported, leading to N-aminosulfonamides in good yields. Not only triethoxy(aryl)silanes but also triethoxy(alkyl)silanes are compatible during the process of insertion of sulfur dioxide. Additionally, diethoxydiarylsilanes are suitable under the conditions as well.