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Updated: Jul 2, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

Trisindoline synthesis and anticancer activity.

Miyoun Yoo¹, Sang-Un Choi, Ki Young Choi

¹Department of Biology, Yonsei University, 134 Shinchon, Seoul 120-749, Republic of Korea.

Biochemical and Biophysical Research Communications

|September 2, 2008

Summary

Researchers discovered trisindoline, a novel compound with potent anticancer activity. This compound effectively targets multidrug-resistant (MDR) cancer cells, offering a promising new avenue for cancer therapy.

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Published on: January 21, 2020

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Last Updated: Jul 2, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

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Published on: February 9, 2021

A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones

A Direct, Regioselective and Atom-Economical Synthesis of 3-Aroyl-N-hydroxy-5-nitroindoles by Cycloaddition of 4-Nitronitrosobenzene with Alkynones

Published on: January 21, 2020

Area of Science:

Biochemistry
Molecular Biology
Pharmacology

Background:

Genetic engineering of Rhodococcus-derived oxygenase in E. coli.
Production of indigo metabolites with cytotoxic properties.

Purpose of the Study:

Isolate and identify the cytotoxic agent from engineered E. coli.
Evaluate the efficacy of the isolated compound against cancer cells, including multidrug-resistant (MDR) lines.

Main Methods:

Bioactivity-guided fractionation of indigo metabolites.
In vitro cytotoxicity assays using parental and MDR cancer cell lines.
Assessment of resistance to P-glycoprotein overexpression.

Main Results:

Trisindoline isolated as the primary cytotoxic agent.
Trisindoline demonstrated potent in vitro cytotoxicity against cancer cells.
Trisindoline exhibited similar efficacy against both parental and MDR cancer cells.
Cytotoxicity of trisindoline was unaffected by P-glycoprotein overexpression.

Conclusions:

Trisindoline is a promising candidate for overcoming cancer multidrug resistance.
The compound's resistance to P-glycoprotein makes it valuable for treating MDR cancers.