Casalvieri, Kimberly A.; Matheson, Christopher J.; Warfield, Becka M.; Backos, Donald S.; Reigan, Philip published the artcile< N-Substituted pyrrolopyrimidines and purines as p90 ribosomal S6 protein kinase-2 (RSK2) inhibitors>, Electric Literature of 229009-40-9, the main research area is pyrrolopyrimidine preparation antitumor RSK2 inhibition SAR; purine preparation antitumor RSK2 inhibition SAR; Inhibitor; Kinase; RSK; Structure-activity relationship.
In the current study, a series of pyrrolopyrimidines and purines were developed to replace the pteridinone ring of BI-D1870, with a range of N-substituents that extended to the substrate binding site to probe complementary interactions, while retaining the 2,6-difluorophenol-4-amino group to maintain interactions with the hinge domain and the DFG motif. Several compounds inhibited cellular RSK2 activity and compounds that uncoupled cellular RSK2 inhibition from potent cytotoxicity in the MOLM-13 AML cell line were identified . These N-substituted probes revealed an opportunity to further examine substituents that extend from the ATP- to the substrate-binding site may confer improved RSK potency and selectivity.
Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Electric Literature of 229009-40-9.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics