1899-94-1Relevant articles and documents
Multiprotein Dynamic Combinatorial Chemistry: A Strategy for the Simultaneous Discovery of Subfamily-Selective Inhibitors for Nucleic Acid Demethylases FTO and ALKBH3
Das, Mohua,Yang, Tianming,Dong, Jinghua,Prasetya, Fransisca,Xie, Yiming,Wong, Kendra H. Q.,Cheong, Adeline,Woon, Esther C. Y.
, p. 2854 - 2867 (2018)
Dynamic combinatorial chemistry (DCC) is a powerful supramolecular approach for discovering ligands for biomolecules. To date, most, if not all, biologically templated DCC systems employ only a single biomolecule to direct the self-assembly process. To expand the scope of DCC, herein, a novel multiprotein DCC strategy has been developed that combines the discriminatory power of a zwitterionic “thermal tag” with the sensitivity of differential scanning fluorimetry. This strategy is highly sensitive and could differentiate the binding of ligands to structurally similar subfamily members. Through this strategy, it was possible to simultaneously identify subfamily-selective probes against two clinically important epigenetic enzymes: FTO (7; IC50=2.6 μm) and ALKBH3 (8; IC50=3.7 μm). To date, this is the first report of a subfamily-selective ALKBH3 inhibitor. The developed strategy could, in principle, be adapted to a broad range of proteins; thus it is of broad scientific interest.
Electrochemically generatedN-iodoaminium species as key intermediates for selective methyl sulphonylimination of tertiary amines
Huang, Binbin,Yang, Chao,Zhou, Jia,Xia, Wujiong
supporting information, p. 5010 - 5013 (2020/05/18)
Reported herein is a straightforward protocol for approachingN-sulphonylamidinesviaan electricity-driven, iodine-mediated cross dehydrogenative condensation (CDC) between sulphonamides and tertiary amines, which features exclusive N-CH3selectivity for the amine partners. Mechanistic studies indicate that anin situgeneratedN-iodoaminium species serves as the key intermediate.
Manganese-Catalyzed N-Alkylation of Sulfonamides Using Alcohols
Reed-Berendt, Benjamin G.,Morrill, Louis C.
, p. 3715 - 3724 (2019/03/30)
An efficient manganese-catalyzed N-alkylation of sulfonamides has been developed. This borrowing hydrogen approach employs a well-defined and bench-stable Mn(I) PNP pincer precatalyst, allowing benzylic and simple primary aliphatic alcohols to be employed as alkylating agents. A diverse range of aryl and alkyl sulfonamides undergoes mono-N-alkylation in excellent isolated yields (32 examples, 85% average yield).
