Related Experiment Video
Updated: Oct 20, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Current Status of Novel Pyridine Fused Derivatives as Anticancer Agents: An Insight into Future Perspectives and
Ajay Manaithiya1, Ozair Alam1, Vrinda Sharma1
1Medicinal Chemistry and Molecular Modelling Lab, Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi-110062, India.
Abstract:
Cancer is a heterogeneous disease characterized by an abnormal and uncontrolled division of the cells leading to tumors that invade the adjacent normal tissues. After cardiovascular diseases, it is the second most prevalent disease accounting for one in every six deaths worldwide. This alarming rate thus, demands an urgent need to investigate more effective drugs to combat the said disease. Oxygen and nitrogen-based heterocyclic compounds have shown remarkable therapeutic activity towards several diseases, including cancer. In this review, we have attempted to summarize the work done in the last decade (2009-2019), highlighting the anticancer activity of pyrido fused fivemembered heterocyclic ring derivatives. Additionally, we have focused on seven heterocyclic pyridine fused rings: Imidazopyridine, Triazolopyridine, Pyrrolopyridine, Pyrazolopyridines, Thienopyridine, and Isoxazolopyridine. A total of forty-nine compounds have been studied based on their invitro cytotoxic activity and their structure-activity relationship, underlining the anticancer activity of their various pharmacophores and substituents. This review, therefore, aims to draw the attention of the researchers worldwide towards the enormous scope of development of heterocyclic drug compounds, focussing mainly on pyrido fused five-membered heterocyclic rings as anticancer drugs.
Insights
Pyrido fused five-membered heterocyclic compounds show significant anticancer potential. This review highlights their therapeutic activity and structure-activity relationships for developing novel cancer drugs.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Cancer is a leading global cause of death, necessitating novel therapeutic strategies.
- Heterocyclic compounds, particularly oxygen and nitrogen-based ones, exhibit promising anticancer properties.
Purpose of the Study:
- To review the anticancer activity of pyrido fused five-membered heterocyclic ring derivatives.
- To summarize structure-activity relationships of these compounds from 2009-2019.
Main Methods:
- Literature review focusing on pyrido fused five-membered heterocycles.
- Analysis of in vitro cytotoxic activity and structure-activity relationships (SAR) of 49 compounds.
Main Results:
- Identified seven key heterocyclic pyridine fused rings with anticancer potential: Imidazopyridine, Triazolopyridine, Pyrrolopyridine, Pyrazolopyridines, Thienopyridine, and Isoxazolopyridine.
- Highlighted the role of various pharmacophores and substituents in determining anticancer efficacy.
Conclusions:
- Pyrido fused five-membered heterocyclic rings represent a promising scaffold for developing new anticancer drugs.
- Further research into these compounds could lead to effective cancer therapies.
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Five-Membered Heterocyclic Aromatic Compounds: Overview
Targeted Cancer Therapies
There are several types of targeted therapies against...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...

