One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 637-01-4, Name is N1,N1,N4,N4-Tetramethylbenzene-1,4-diamine dihydrochloride, formurla is C10H18Cl2N2. In a document, author is Halin, Emilie, introducing its new discovery. Category: amides-buliding-blocks.
Ugi multicomponent-reaction: Syntheses of cytotoxic dehydroabietylamine derivatives
Isocyanide-based multicomponent reactions – especially the standard four component Ugi reaction – provide an easy and powerful access to compounds with an auspicious pharmacological potential. Therefore, a set of 16 novel derivatives of the diterpene dehydroabietylamine was synthesized by the Ugi-4CR. The subsequent screening of the synthesized alpha-acylamino carboxamides in colorimetric sulforhodamine B assays revealed an in vitro cytotoxicity towards several human tumor cell lines. Particularly, the rhodamine B conjugates 14-16 showed a remarkable cytotoxic activity, characterized by EC50 values in a low three-digit nanomolar range. The screening of rhodamine B amide 17 that was obtained for comparison by a Schotten-Baumann reaction showed that the linkage of the rhodamine B moiety and the diterpene influences significantly its cytotoxic potency. While 14 was highly cytotoxic and acted as a mitocan, compound 17 was not cytotoxic a all. This observation underlines the importance of the type of coupling between the diterpene and the rhodamine part. The presence of a rhodamine B moiety in the molecules doesn’t necessarily guarantee that the compound is cytotoxic.
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