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Updated: Dec 17, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Thiophene-based derivatives as anticancer agents: An overview on decade's work
Archna1, Shelly Pathania1, Pooja A Chawla1
1Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga 142001, Punjab, India.
Thiophene derivatives are promising anticancer agents, targeting various cancer pathways. This review details their synthesis, biological activity, and structure-activity relationships for drug development.
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Heterocyclic compounds are crucial in drug discovery, particularly for developing anticancer agents.
- Thiophene, a sulfur-containing heterocycle, is a well-explored scaffold for anticancer drug development.
- Thiophene analogs exhibit diverse biological activities by targeting cancer-specific proteins and signaling pathways.
Purpose of the Study:
- To review thiophene-based molecules as anticancer agents.
- To focus on synthetic methodologies, biological profiles, and structure-activity relationship (SAR) studies.
- To include granted patents for thiophene-containing anticancer compounds.
Main Methods:
- Literature review of scientific publications and patents.
- Analysis of synthetic routes for thiophene derivatives.
- Evaluation of biological data and SAR studies for anticancer activity.
Main Results:
- Thiophene analogs demonstrate significant anticancer potential through various mechanisms.
- Diverse substitution patterns on the thiophene ring influence target specificity and efficacy.
- Numerous thiophene derivatives have been patented for their anticancer properties.
Conclusions:
- Thiophene scaffolds are valuable in the development of novel anticancer therapeutics.
- Understanding SAR is key to designing potent and selective thiophene-based anticancer drugs.
- Further research into thiophene derivatives holds promise for future cancer treatments.
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