77278-38-7Relevant articles and documents
Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors
Velnati, Suresh,Massarotti, Alberto,Antona, Annamaria,Talmon, Maria,Fresu, Luigia Grazia,Galetto, Alessandra Silvia,Capello, Daniela,Bertoni, Alessandra,Mercalli, Valentina,Graziani, Andrea,Tron, Gian Cesare,Baldanzi, Gianluca
, p. 96 - 108 (2020)
A series of analogues of Amb639752, a novel diacylglycerol kinase (DGK) inhibitor recently discovered by us via virtual screening, have been tested. The compounds were evaluated as DGK inhibitors on α, θ, and ζ isoforms, and as antagonists on serotonin re
Direct Amidation of Esters by Ball Milling**
Barreteau, Fabien,Battilocchio, Claudio,Browne, Duncan L.,Godineau, Edouard,Leitch, Jamie A.,Nicholson, William I.,Payne, Riley,Priestley, Ian
supporting information, p. 21868 - 21874 (2021/09/02)
The direct mechanochemical amidation of esters by ball milling is described. The operationally simple procedure requires an ester, an amine, and substoichiometric KOtBu and was used to prepare a large and diverse library of 78 amide structures with modest to excellent efficiency. Heteroaromatic and heterocyclic components are specifically shown to be amenable to this mechanochemical protocol. This direct synthesis platform has been applied to the synthesis of active pharmaceutical ingredients (APIs) and agrochemicals as well as the gram-scale synthesis of an active pharmaceutical, all in the absence of a reaction solvent.
Catalytic N-Acylation of Cyclic Amines by Arylglyoxylic Acids via Radical-Radical Cross-Coupling
Bhadra, Sukalyan,Gupta, Aniket,Kumar Singh, Anupam,Rahaman, Ajijur
supporting information, p. 2198 - 2202 (2021/07/22)
A methodical mechanistic investigation allowed for the catalytic N-acylation of secondary cyclic amine counterparts by arylglyoxylic acids through radical-radical coupling. The reaction proceeds via a twofold SET-promoted Cu(I)/Cu(II) catalytic cycle under mild conditions. An analogous reaction variant allows for the N-acylation in a one-pot fashion directly starting from a secondary cyclic amine even in the presence of a second amine or hydroxy group.
Design, synthesis and antitumor evaluation of new 1,8-naphthalimide derivatives targeting nuclear DNA
Liang, Gui-Bin,Wei, Jian-Hua,Jiang, Hong,Huang, Ri-Zhen,Qin, Jing-Ting,Wang, Hui-Ling,Wang, Heng-Shan,Zhang, Ye
, (2020/11/02)
Four series of new 3-nitro naphthalimides derivatives, 4(4a?4f), 5(5a?5i), 6(6a?6e) and 7 (7a?7j), were designed and synthesized as antitumor agents. Methyl thiazolyl tetrazolium (MTT) screening assay results revealed that some compounds displayed effecti