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Related Experiment Video

Updated: Feb 14, 2026

Murine Model of Leukemia Relapse to Induction Chemotherapy for Acute Lymphoblastic Leukemia

Murine Model of Leukemia Relapse to Induction Chemotherapy for Acute Lymphoblastic Leukemia

Published on: October 17, 2025

Novel vitexin-inspired scaffold against leukemia.

Taotao Ling¹, Walter Lang¹, Xiang Feng¹

¹Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, TN 38105-3678, USA.

European Journal of Medicinal Chemistry

|February 7, 2018

Summary

Researchers identified vitexin, a natural compound, showing promise against childhood acute lymphoblastic leukemia (ALL). A new library of vitexin-inspired compounds demonstrated potent anti-leukemia activity with minimal toxicity, offering a novel therapeutic scaffold.

Keywords:

Cdk inhibitor Quinolin-4(1H)-one Reactive oxygen species Vitexin

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Published on: February 9, 2016

Area of Science:

Natural Product Chemistry
Medicinal Chemistry
Cancer Biology

Background:

Acute lymphoblastic leukemia (ALL) is the most common childhood cancer.
Relapsed ALL presents a significant challenge with poor patient prognosis.
Identifying novel therapeutic agents is crucial for improving ALL treatment outcomes.

Purpose of the Study:

To discover new compound leads for acute lymphoblastic leukemia (ALL) treatment.
To synthesize and evaluate a library of vitexin-inspired compounds for enhanced anti-leukemia activity.
To investigate the potential mechanism of action of novel ALL-targeting compounds.

Main Methods:

Phenotypic screening of terrestrial natural product fractions against ALL cellular models.
Synthesis of a vitexin-inspired compound library using a one-pot condensation reaction.
Evaluation of compound cytotoxicity and anti-proliferative activity in ALL and normal cell lines.
Computational studies to predict mechanism of action (e.g., CDK inhibition).

Main Results:

Vitexin identified as a hit compound with activity against pre-B cell ALL models (EC50 = 30 μM).
Novel 4-quinolone core heterocycles with N-sulfonamide synthesized, showing potent anti-ALL activity (EC50 = 0.3-10 μM) and low toxicity.
Computational studies suggest compounds are potential CDK inhibitors.
Compounds induced apoptosis, cell cycle arrest (G0/G1 and G2/M), and ROS production in cancer cells.

Conclusions:

Vitexin serves as a promising starting point for ALL drug discovery.
The synthesized vitexin-inspired compounds represent a novel molecular scaffold with significant therapeutic potential against ALL.
These compounds exhibit a multi-pronged mechanism of action, including CDK inhibition, apoptosis induction, and cell cycle arrest.