Synthesis and application of isoindole-1, 3-dione derivative as RSK2 inhibitor
A C1-C3, purpose-based technology, applied in the synthesis of isoindoledione compounds and in the fields of medicinal chemistry and pharmacotherapeutics, to achieve the effect of inhibiting growth
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Embodiment 1
[0068] The synthetic methods of some 2-substituted-isoindole-1,3 diketones with structural modification are as follows:
[0069] Main instruments and reagents:
[0070] Bruker company AV-400MHz nuclear magnetic resonance instrument (DMSO-d 6 , CDCl 3 as the solvent and TMS as the internal standard). All reagents were commercially pure or analytically pure.
[0071] 2-(anilinomethyl)-isoindole-1,3 dione---synthesis of compound 1:
[0072]
[0073] Weigh phthalimide (300mg, 2.0mmol) and 37% formaldehyde solution (0.2mL, 2.0mmol) into a 25mL round bottom bottle, add 4mL of 80% ethanol solution, and reflux at 80°C , after the reaction solution is clear and transparent, take aniline (209mg, 2.2mmol) and dissolve it in 1mL of 80% ethanol solution, then add it to the above reaction solution, TLC plate tracking reaction process, until the raw materials are completely consumed, the reaction solution is cooled After cooling to room temperature and standing overnight, a large amo...
Embodiment 2
[0099] The in vitro inhibitory effect test of the compounds provided by the invention on RSK2 kinase activity is as follows:
[0100] Screening method: S6 peptide (AKRRLSSLRA) is phosphorylated in the presence of RSK2 and consumes ATP to generate ADP, and the enzyme activity is determined by detecting ADP. Screening target: RSK2 (cancer target).
[0101] The activity of RSK2 is determined by detecting the ADP produced by the kinase reaction process to determine the activity of the enzyme. The ADP QuestTM Assay kit from DiscoverRx can be used to detect the amount of ADP accumulated during the kinase reaction. In a 40 μl reaction system, 25 μM S6 peptide (AKRRLSSLRA) substrate and 10 ng enzyme were included. Compounds and enzymes were incubated at room temperature for 20 min. Then 10 μl of ATP (10 μM final concentration) was added to start the reaction. After reacting at room temperature for 1 hour, 20 μl of reagent A and 40 μl of reagent B were added, and after incubation a...
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