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Topoisomerase I and II Inhibitors: A Patent Review

Arshdeep Singh, Navdeep Kaur, Gurpreet Singh

  • 1Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, India. ss.gq2009@gmail.com.

Recent Patents on Anti-Cancer Drug Discovery
|July 25, 2016
PubMed
Abstract

Insights

Topoisomerase enzymes are crucial for DNA management and cell survival. Inhibiting them, particularly with novel nitrogen-containing heteroaromatic compounds, shows promise for developing new anticancer drugs targeting DNA damage and apoptosis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Topoisomerases are nuclear enzymes essential for managing DNA topology during cellular processes.
  • Inhibition of topoisomerases disrupts DNA ligation, leading to strand breaks and programmed cell death (apoptosis).

Purpose of the Study:

  • To review patent literature up to 2016 on topoisomerase inhibitors for anticancer drug development.
  • To highlight structurally diverse inhibitors including camptothecin analogs, lamellarins, and synthetic pyridines.

Main Methods:

  • Compilation and analysis of patent literature focusing on topoisomerase I, II, and dual inhibitors.
  • Review of chemical structures and their relationship to inhibitory activity.

Main Results:

  • Nitrogen-containing heteroaromatic compounds, especially fused N-heterocycles, demonstrate significant topoisomerase inhibitory potential.
  • Naphthyridinone and indenoisoquinoline derivatives show potent activity against topoisomerase I.

Conclusions:

  • Fused N-heterocycles represent a promising class of compounds for anticancer therapy, potentially used alone or in combination.
  • Naphthyridinone and indenoisoquinoline derivatives warrant further preclinical and clinical investigation as future drug candidates.

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