96483-83-9Relevant articles and documents
Pyruvate kinase activators for use in therapy
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Page/Page column 178, (2016/08/29)
Described herein are methods for using compounds that activate pyruvate kinase.
Synthesis and antiproliferative properties of N3/8-disubstituted 3,8-diazabicyclo[3.2.1]octane analogues of 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl-piperazine
Filosa, Rosanna,Peduto, Antonella,de Caprariis, Paolo,Saturnino, Carmela,Festa, Michela,Petrella, Antonello,Pau, Amedeo,Pinna, Gerard Aime,La Colla, Paolo,Busonera, Bernardetta,Loddo, Roberta
, p. 293 - 306 (2008/02/01)
A series of novel N3/8-disubstituted-3,8-diazabicyclo[3.2.1]octanes in order to improve the in vitro activity of the prototype 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridyl-4-yl)methylpiperazine (1) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines. Compounds 2a,b,f and m demonstrated not only growth-inhibitory activities against leukemia cancer cells, but also fairly good activities against the growth of certain solid tumors. Among them, 2a is the most potent one with IC50 values in the low micromolar range. Moreover, compound 2a has been selected for in vitro testing on MCF-7 cell to evaluate the mode of action of this lead compound.
Tandem cyclisation and [2,3]-Stevens rearrangement to 2-substituted pyrrolidines
Smith, Stephen C,Bentley, Philip D
, p. 899 - 902 (2007/10/03)
Reaction of N-methylallylamine with diethyl meso-2,5-dibromoadipate in DMF at ambient temperature in the presence of potassium carbonate led directly to the two diastereomers of diethyl 2-allyl-N-methylpyrrolidine-2,5-dicarboxylate. The reaction proceeds via a [2,3]-sigmatropic Stevens rearrangement, which occurred spontaneously under the reaction conditions. This gave a higher yield under milder conditions than the traditional Stevens reaction of diethyl N-allylpyrrolidine-2,5-dicarboxylate with iodomethane. The sequence was a key step in the synthesis of a series of analogues of the alkaloid stemofoline.