In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Development of peptide epoxyketones as selective immunoproteasome inhibitors, published in 2021-10-05, which mentions a compound: 120099-61-8, mainly applied to epoxyketone peptide synthesis peptidomimetic immunoproteasome inhibitor structure activity; antitumor agent drug design mol docking hydrogen bond chirality; isocyanate peptide coupling; Epoxyketones; Immunoproteasome inhibitor; Multiple myeloma; Selectivity, Recommanded Product: (S)-3-Methoxypyrrolidine.
A series of epoxyketone analogs with varying N-caps and P3-configurations were designed, synthesized and evaluated. We found that D-Ala in P3 was crucial for β5i selectivity over β5c. Notably, compounds (I) (R1 = II) (β5i IC50 = 26.0 nM, 25-fold selectivity) and I (r1 = III) (β5i IC50 = 25.1 nM, 24-fold selectivity) with the D-configuration at P3 were the most selective inhibitors. Although I (R1 = II and III) showed only moderate anti-proliferative activity against RPMI-8226 and MM.1S cell lines, based on our experiments, it indicates that the inhibition of β5i alone is not sufficient to exert anticancer effects and may rely on the complementary inhibition of β1i, β5c and β5i. These data further increase our understanding of immunoproteasome inhibitors in hematol. malignancies.
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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia