149990-27-2Relevant articles and documents
A Domino 10-Step Total Synthesis of FR252921 and Its Analogues, Complex Macrocyclic Immunosuppressants
Chen, Yong,Coussanes, Guilhem,Souris, Caroline,Aillard, Paul,Kaldre, Dainis,Runggatscher, Kathrin,Kubicek, Stefan,Di Mauro, Giovanni,Maryasin, Boris,Maulide, Nuno
, p. 13772 - 13777 (2019)
FR252921, FR252922, and FR256523 are a family of potent macrocyclic polyene immunosuppressive agents with a novel mode of action. However, the lack of an efficient and flexible synthesis has hindered further biological studies, mostly due to the fact that the natural products appear to be kinetic isomers regarding the triene moiety. Herein, we report the development and application of an unprecedented, unique domino Suzuki-Miyaura/4π-electrocyclic ring-opening macrocyclization, resulting in a concise, unified, and stereoselective synthetic route to these complex targets in only 10 steps. This in turn enables ready access to a range of unnatural analogues, among which several compounds showed inhibition of T-lymphocyte proliferation at levels equal or superior to those of the natural products themselves.
HYDROXY-PYRIDINALDOXIME SCAFFOLDS
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, (2022/03/22)
The present invention relates to a compound of formula (I). It also relates to a pharmaceutical composition comprising at least one compound of formula (I) and at least one pharmaceutically acceptable support. Finally, it relates to the use of such a compound as a medicine, preferably in the treatment of a nervous and/or respiratory failure due to intoxication with at least one organophosphorous nerve agent; in the treatment of neurological diseases such as Alzheimer's disease; and/or in the treatment of cancer.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00962; 001987-001989, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.