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Updated: Apr 3, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Recent Advances in Anticancer Chemotherapeutics based upon Azepine Scaffold
Sarbjit Singh, Jail Goo, Veeraswamy Gajulapati
1College of Pharmacy, Dongguk University-Seoul, Goyang, 410-820, Korea. kaylee@dongguk.edu.
Azepine-based compounds, a type of heterocyclic anti-cancer agent, show growing promise. This review covers recent advancements in developing these compounds for cancer treatment since 2000.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Heterocyclic compounds are crucial in developing novel anti-cancer agents.
- Azepine derivatives are emerging as a significant class of anti-cancer compounds.
- Research in this area has intensified due to the potential of azepine scaffolds.
Purpose of the Study:
- To review recent advancements in azepine-based anti-cancer compounds.
- To highlight key developments in the field since the year 2000.
- To provide an overview of the current landscape of azepine-based anti-cancer drug discovery.
Main Methods:
- Literature search of scientific databases (e.g., PubMed, Scopus, Web of Science).
- Focus on peer-reviewed articles, reviews, and patents published since 2000.
- Analysis of synthetic strategies, structure-activity relationships, and biological evaluations of azepine compounds.
Main Results:
- Identification of various azepine-based compounds with significant anti-cancer activity.
- Discussion of diverse synthetic routes employed for azepine scaffold construction.
- Summary of key structural modifications and their impact on efficacy and selectivity.
Conclusions:
- Azepine-based compounds represent a promising avenue for novel anti-cancer drug development.
- Continued research into azepine derivatives is warranted to explore their full therapeutic potential.
- The field has witnessed substantial progress, with numerous compounds showing potential for clinical application.
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