These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis and biological evaluation of curcumin derivatives modified with α-amino boronic acid as proteasome inhibitors.
    Author: Zhang W, Bai H, Han L, Zhang H, Xu B, Cui J, Wang X, Ge Z, Li R.
    Journal: Bioorg Med Chem Lett; 2018 Aug 01; 28(14):2459-2464. PubMed ID: 29886021.
    Abstract:
    Curcumin is a well-known pharmacophore and some of its derivatives are shown to target 20S proteasome recently. In this report, we designed and synthesized two series of curcumin derivatives modified with different α-amino boronic acids as potent proteasome inhibitors. The synthesized compounds were evaluated for their cytotoxic activities against HCT116 cells, and the results showed that all of them exhibited excellent cell growth inhibitory activity comparing with curcumin, with the IC50 values varying from 0.17 μM to 1.63 μM. Compound II-2F with free boronic acid was assayed for its proteasome inhibitory activity and the results indicated that II-2F exhibited more potent inhibitory activity against ChT-L with high subunit selectivity than any other reported curcumin derivatives.
    [Abstract] [Full Text] [Related] [New Search]