Recent progress in topoisomerase inhibitors as anticancer agents: Research and design strategies for Topo I and II...

Area of Science:

• Biochemistry
• Molecular Biology
• Oncology

Background:

• Topoisomerases (Topo) are vital enzymes for DNA replication, transcription, and repair.
• Topo I and II are essential for tumor cell proliferation and genomic stability.
• Current Topo inhibitors face challenges like drug resistance and toxicity.

Purpose of the Study:

• To review structural and optimization advances in Topo I and II inhibitors over the last five years.
• To focus on catalytic inhibitors and multitarget agents for improved cancer therapy.
• To offer new perspectives for developing safer, more effective small-molecule Topo inhibitors.

Main Methods:

• Systematic review and analysis of recent literature (past five years).
• Focus on structural modifications and optimization strategies.
• Analysis of catalytic and multitargeting approaches for Topo inhibitors.

Main Results:

• Identification of key structural advancements in Topo I and II inhibitors.
• Evaluation of progress in developing catalytic and multitargeting agents.
• Analysis of strategies to mitigate drug resistance and toxicity.

Conclusions:

• Significant progress has been made in developing novel Topo inhibitors.
• Catalytic and multitargeting agents show promise for enhanced efficacy and reduced toxicity.
• Further research into small-molecule Topo inhibitors is crucial for advancing cancer therapy.