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Published on: February 9, 2021
A Review on Anticancer Activities of Thiophene and Its Analogs
Raghav Mishra1, Nitin Kumar2, Isha Mishra1
1Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, 281406, India.
Abstract:
Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold, which, because of their appreciable diversity in biological activities, has drawn the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher's consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structure-activity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through the activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives, whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.
Insights
Thiophene derivatives show significant potential as anticancer agents, offering diverse biological activities and novel therapeutic mechanisms. This review highlights their role in developing new cancer treatments with improved efficacy and reduced toxicity.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Oncology
Background:
- Cancer remains a leading cause of mortality globally, necessitating the development of novel and less toxic therapies.
- Thiophene and its derivatives are recognized for their diverse biological activities, including antioxidant, anti-inflammatory, antimicrobial, and anticancer properties.
- The structural versatility of thiophene scaffolds allows for significant modulation of activity through substituent modification.
Purpose of the Study:
- To review and promote the anticancer potential of thiophene derivatives as chemotherapeutic agents.
- To explore the structure-activity relationships of thiophene derivatives in cancer therapy.
- To identify key anticancer mechanisms associated with thiophene-based compounds.
Main Methods:
- Literature review of scientific articles focusing on thiophene derivatives and their anticancer activities.
- Analysis of structure-activity relationships to understand the impact of substitutions on efficacy.
- Identification of established anticancer mechanisms of action for thiophene-based compounds.
Main Results:
- Thiophene derivatives exhibit promising anticancer activity against various cancer cell lines.
- Key anticancer mechanisms include topoisomerase inhibition, tyrosine kinase inhibition, tubulin interaction, and apoptosis induction via reactive oxygen species.
- The nature and position of substituents on the thiophene ring significantly influence its biological activity.
Conclusions:
- Thiophene and its derivatives represent a vital scaffold for the development of novel anticancer lead compounds.
- Further research into thiophene-based compounds can lead to the synthesis of effective chemotherapeutic agents.
- The diverse biological activities and identified mechanisms underscore the therapeutic promise of thiophene derivatives in cancer treatment.

