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Updated: Mar 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
A Comprehensive Review of N-Heterocycles as Cytotoxic Agents
Dinesh Kumar, Subheet Kumar Jain1
1Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab- 143005, India.
Abstract:
Scientific community is striving to understand the role of heterocycles and fused heterocycles in drug discovery programme due to its impact on multi-drug resistance (MDR) of anticancer drugs. Architecting of various scaffolds for cancer treatment has become gradually increased in many years. Till now there is no treatment which is so proficient that it can cure the cancer from the roots. Hence, it is very necessary to design novel anticancer agents with minimum side effects. Synthesis of hybrids from natural leads is one of the rationale approaches in medicinal chemistry. It remains a big challenge to invent new efficient drugs to beat cancer. The design and synthesis of fused molecules as anticancer agents is one of the great innovations of modern era. In drug discovery archetype, a variety of heterocycles have been considered for the development of novel lead compounds. This article presents some recent advancements in the field of anticancer heterocyclic agents all around the world and also attracted the structure activity relationship along with the structure of the most promising molecules along with IC50 values against various human cancer cell lines.
Insights
Researchers are exploring novel heterocyclic compounds for anticancer drug discovery to combat multi-drug resistance (MDR). This study highlights recent advancements in designing effective anticancer agents with minimal side effects.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Organic Chemistry
Background:
- The scientific community is investigating heterocycles and fused heterocycles for their impact on multi-drug resistance (MDR) in anticancer drugs.
- Developing effective cancer treatments with minimal side effects remains a significant challenge.
- Novel drug design is crucial to overcome cancer's complexity and limitations of current therapies.
Purpose of the Study:
- To review recent advancements in anticancer heterocyclic agents globally.
- To explore the structure-activity relationships (SAR) of promising anticancer molecules.
- To present structures and IC50 values of novel anticancer compounds against various human cancer cell lines.
Main Methods:
- Literature review of recent developments in anticancer heterocyclic agents.
- Analysis of structure-activity relationships (SAR) for identified compounds.
- Compilation of IC50 values for promising molecules against diverse cancer cell lines.
Main Results:
- Identification of promising heterocyclic scaffolds with potential anticancer activity.
- Correlation of specific structural features with observed anticancer efficacy.
- Presentation of detailed IC50 data for selected compounds against various human cancer cell lines.
Conclusions:
- Heterocyclic and fused heterocyclic compounds represent a vital area for developing novel anticancer agents.
- Understanding SAR is key to designing more potent and selective anticancer drugs.
- Continued research into novel heterocyclic structures is essential for advancing cancer therapy.
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