689254-66-8Relevant academic research and scientific papers
CYCLIC SULFAMIDES FOR INHIBITION OF GAMMA-SECRETASE
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Page 18, (2008/06/13)
Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
Synthesis and Antineoplastic Activity of Bisoxy>methyl>-Substituted 3-Pyrrolines as Prodrugs of Tumor Inhibitory Pyrrole Bis(carbamates)
Anderson, Wayne K.,Milowsky, Arnold S.
, p. 2241 - 2249 (2007/10/02)
A series of bispyrrolines 2-4 were synthesized from either the appropriate α-silylated iminium salt, or an aziridine, or a 2H-azirine in a sequence involving 1,3-dipolar cycloaddition reactions.The antineoplastic activities of the pyrrolines were compared to the corresponding pyrroles.The C-2 gem-dimethyl-substituted pyrroline, 4, which cannot be converted to the pyrrole in vivo, was inactive.The activity of the 2-phenyl-substituted pyrrolines 3 was markedly dependent on the nature of the phenyl substituent, although the correspondingphenylpyrroles all showed comparable activity.The differences in the activities of the pyrrolines 3 may be due to the rate of metabolic conversion of the pyrroline to the pyrrole.Electron-withdrawing substituents on the phenyl ring appear to retard this process.
