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Updated: Dec 15, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

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Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview

Damanpreet K Lang1, Rajwinder Kaur1, Rashmi Arora1

  • 1Chitkara College of Pharmacy, Chitkara University, Punjab, India.

Anti-Cancer Agents in Medicinal Chemistry
|July 7, 2020
PubMed
Abstract

Insights

Nitrogen-containing heterocycles are crucial building blocks for developing novel anti-cancer drugs with fewer side effects. This review compiles a dataset of these vital compounds used in chemotherapy and kinase inhibitors.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Drug Discovery

Background:

  • Cancer is a leading global cause of death, necessitating new treatments with minimal side effects.
  • Current cancer therapies include chemotherapy, radiotherapy, surgery, and immunotherapy, often involving kinase inhibitors.
  • Many anti-cancer drugs utilize kinase inhibition as their core mechanism.

Purpose of the Study:

  • To compile a dataset of nitrogen-containing heterocyclic anti-cancer drugs.
  • To highlight the importance of nitrogen heterocycles in developing novel anti-cancer agents.
  • To provide an overview of active nitrogen-containing heterocyclic compounds as anti-cancer agents.

Main Methods:

  • Conducted a structural search across major scientific databases (PubMed, Scopus, Science Direct) and regulatory sites (USFDA).
  • Collected and reviewed peer-reviewed research and review articles.
  • Categorized, analyzed, and synthesized retrieved information for the review.

Main Results:

  • Nitrogen-based heterocycles constitute approximately 60% of unique small-molecule drugs approved by the FDA.
  • Identified several key nitrogen-containing heterocyclic anti-cancer drugs, including Imatinib, Gefitinib, and Sunitinib.
  • Emphasized the role of these heterocycles as fundamental structures in chemotherapy agents.

Conclusions:

  • Nitrogen-containing heterocyclic compounds are essential scaffolds in modern anti-cancer drug design.
  • These compounds offer a promising avenue for developing more effective cancer therapies with reduced adverse effects.
  • The compiled dataset serves as a valuable resource for researchers in medicinal chemistry and oncology.
Keywords:
Anti-cancerFDA approved drugsayvakitcopiktraerleadalorbrenanitrogen heterocyclestazverik

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