1072-44-2Relevant articles and documents
METASTIN DERIVATIVE AND USE THEREOF
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, (2011/06/10)
The invention provides a stable metastin derivative having excellent biological activities (a cancer metastasis-inhibiting activity, a cancer proliferation-inhibiting activity, a gonadotropin secretion-promoting activity, a sex hormone secretion-promoting activity, etc.). By replacing the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, the blood stability and solubility of the metastin derivative can be more improved, the gel tendency of the metastin derivative can be reduced, the pharmacokinetics of the metastin derivative can be improved, and the metastin derivative can exhibit an excellent cancer metastasis-inhibiting activity and cancer proliferation-inhibiting activity. The metastin derivative can also exhibit a gonadotropin secretion-inhibiting activity, a sex hormone secretion-inhibiting activity, etc.
Acid-Catalyzed Decomposition of 1-Alkyltriazolines: A Mechanistic Study
Smith, Richard H.,Wladkowski, Brian D.,Taylor, Jesse E.,Thompson, Erin J.,Pruski, Brunon,et al.
, p. 2097 - 2103 (2007/10/02)
1-Alkyltriazolines are five-membered cyclic triazenes containing the unusual Z-configuration for the triazene moiety.The hydrolytic decomposition of these compounds in aqueous or mixed acetonitrile-aqueous buffers leads predominantly to the formation of the corresponding 1-alkylaziridines and lesser amounts of 2-(alkylamino)ethanols, alkylamines, and acetaldehyde.The latter two products presumably result from hydrolysis of a rearrangement produkt, N-ethylidenealkylamine.Neither the nature of the 1-alkyl group nor the pH of the medium greatly influences the product distribution, although decomposition in purely aqueous buffers slightly reduces the aziridine yields.The rate of hydrolysis of 1-alkyltriazolines is about twice as fast as that of the analogous acyclic 1,3,3-trialkyltriazenes and varies in the order tert-butyl > isopropyl > ethyl > butyl > methyl > propyl > benzyl.The mechanism of the decomposition is specific acid-catalyzed (A1) involving rapid reversible protonation followed by rate-limiting formation of a 2-(alkylamino)ethyldiazonium ion.The slopes of the log kobs versus pH plots are near -1.0.The solvent deuterium isotope effect, kH2O/kD2O, is in all cases methyl > ethyl.
15N CHEMICAL SHIFTS IN AZIRIDINES
Liepin'sh, E. E.,Trapentsier, P. T.,Kalvin'sh, I. Ya.
, p. 1106 - 1109 (2007/10/02)
For a number of 1-substituted aziridines and also some 1,2-disubstituted aziridines it has been shown that electron-donating substituents on the nitrogen atom produce a downfield shift of the 15N resonance.The 15N chemical shifts of aziridines correlate with the 15N shifts in N,N-dimethylamines and primary amines as well as with the 17O shifts in oxiranes.A correlation is also observed between the 15N chemical shifts and the electronegativity of the substituents on the nitrogen atom.
