Catecholic flavonoids acting as telomerase inhibitors

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Updated: Aug 20, 2026

Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
09:50

Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade

Published on: August 14, 2019

Maria Menichincheri1, Dario Ballinari, Alberto Bargiotti

  • 1Department of Chemistry, BU-Nerviano Medical Sciences, Viale Pasteur 10, 20014 Nerviano (MI), Italy. maria.menichincheri@nervianoms.com

Journal of Medicinal Chemistry
|December 14, 2004
PubMed

Insights

Researchers discovered a new telomerase inhibitor, 7,8,3

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Telomerase is a key target in oncology.
  • Development of novel telomerase inhibitors is crucial for anticancer drug discovery.

Purpose of the Study:

  • To identify novel telomerase inhibitors from polyhydroxylated flavonoids.
  • To optimize lead compounds through medicinal chemistry for enhanced anticancer activity.

Main Methods:

  • Focused screening of polyhydroxylated flavonoids.
  • In vitro activity assessment using Flash-Plate and TRAP assays.
  • Medicinal chemistry optimization and synthesis of structural analogues.

Main Results:

  • Identified 7,8,3',4'-tetrahydroxyflavone as a potent telomerase inhibitor (IC50 = 0.2 microM).
  • Developed new structural analogues with submicromolar potencies.
  • Confirmed in vitro activity through validated assays.

Conclusions:

  • 7,8,3',4'-tetrahydroxyflavone is a promising lead for anticancer drug development.
  • Medicinal chemistry modifications successfully enhanced telomerase inhibitory activity.
  • Optimized analogues represent potential new anticancer agents.

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