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Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Huixin Liang1, Wei Wang2, Fugui Zhu1

  • 1Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.

Bioorganic & Medicinal Chemistry
|May 13, 2022
PubMed

Insights

Novel bis-evodiamine derivatives, inspired by evodiamine, exhibit potent antitumor effects. Compound 13b effectively inhibits HCT116 cell proliferation and migration by inducing apoptosis and cell cycle arrest.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Evodiamine is a natural product with known antitumor properties.
  • There is a need for novel anticancer agents with improved efficacy.
  • Bis-evodiamine derivatives offer a promising structural scaffold for drug discovery.

Purpose of the Study:

  • To design and synthesize novel bis-evodiamine derivatives.
  • To evaluate the in vitro antitumor activity of these compounds.
  • To investigate the mechanism of action of the most potent derivative.

Main Methods:

  • Chemical synthesis of bis-evodiamine derivatives.
  • In vitro cell proliferation and migration assays using HCT116 cells.
  • Flow cytometry to analyze cell cycle distribution and apoptosis.

Main Results:

  • Several synthesized bis-evodiamine derivatives demonstrated significant antitumor activity.
  • Compound 13b showed potent inhibition of HCT116 cell proliferation and migration.
  • Compound 13b induced apoptosis and G2/M cell cycle arrest in HCT116 cells.

Conclusions:

  • Compound 13b is a promising lead compound for developing new antitumor drugs.
  • Bis-evodiamine derivatives represent a viable class of anticancer agents.
  • Further studies are warranted to explore the therapeutic potential of compound 13b.
Keywords:
Antitumor activityApoptosisBis-evodiamineTwin drug

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