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Updated: Jan 31, 2026

Hydrolysis of a Ni-Schiff-Base Complex Using Conditions Suitable for Retention of Acid-labile Protecting Groups
06:44

Hydrolysis of a Ni-Schiff-Base Complex Using Conditions Suitable for Retention of Acid-labile Protecting Groups

Published on: April 6, 2017

10.1K

Discovery of vanadium complexes bearing tridentate schiff base ligands as novel LSD1 inhibitors

Ling-Pan Lu1, Jin-Hai Liu1, Shi-Hong Cen1

  • 1School of Pharmaceutical Sciences, Zhengzhou University of Industrial Technology, Zhengzhou 451199, PR China.

Bioorganic & Medicinal Chemistry Letters
|January 7, 2019
PubMed

Insights

Researchers developed novel vanadium complexes as potential cancer drugs. Complex 2 moderately inhibited Lysine Specific Demethylase (LSD1), an enzyme linked to cancer, offering a new therapeutic avenue.

Area of Science:

  • Biochemistry
  • Epigenetics
  • Medicinal Chemistry

Background:

  • Lysine Specific Demethylase (LSD1) is crucial for epigenetic gene regulation.
  • Aberrant LSD1 expression correlates with human cancer progression and oncogenesis.

Purpose of the Study:

  • To evaluate synthetic vanadium (V) complexes as potential inhibitors of LSD1.
  • To explore novel therapeutic scaffolds for targeting LSD1 in cancer treatment.

Main Methods:

  • Synthesis and characterization of novel vanadium (V) complexes.
  • In vitro evaluation of inhibitory activity against LSD1.
  • Selectivity assessment against Monoamine Oxidase A/B (MAO-A/B).

Main Results:

  • Complex 2 demonstrated moderate inhibitory activity against LSD1 with an IC50 of 19.0 μM.
  • Complex 2 exhibited good selectivity over MAO-A/B.
  • This marks the first report of a vanadium-based LSD1 inhibitor.

Conclusions:

  • Vanadium complex 2 represents a novel class of LSD1 inhibitors.
  • The findings provide a new scaffold for developing targeted cancer therapies by inhibiting LSD1.
Keywords:
AnticancerLSD1MAOVanadium complex

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