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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Coumarin-containing hybrids and their anticancer activities
1Department of Chemistry, Tsinghua University, Beijing, 100084, PR China.
Abstract:
Cancer is the second leading cause of death worldwide, and it results in around 9 million deaths annually. The anticancer agents play an intriguing role in the treatment of cancers, while the severe anticancer scenario and the emergence of drug-resistant especially multidrug-resistant cancers create a huge demand for novel anticancer drugs with different mechanisms of action. The coumarin scaffold is ubiquitous in nature and is a highly privileged motif for the development of novel drugs due to its biodiversity and versatility. Coumarin derivatives can exert diverse antiproliferative mechanisms, and some of them such as Irosustat are under clinical trials for the treatment of various cancers, revealing their potential as putative anticancer drugs. Hybridization of coumarin moiety with other anticancer pharmacophores is a promising strategy to reduce side effects, overcome the drug resistance, and may provide valuable therapeutic intervention for the treatment of cancers. Thus, coumarin-containing hybrids occupy an important position in the development of novel anticancer agents. This review aims to summarize the recent advances made towards the development of coumarin-containing hybrids as potential anticancer agents, covering articles published between 2015 and 2019, and the structure-activity relationship together with mechanisms of action are also discussed.
Insights
Novel coumarin-containing hybrids show promise as anticancer agents, offering new mechanisms to combat drug resistance and reduce side effects in cancer treatment.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Cancer is a leading global cause of death, necessitating novel therapeutic strategies.
- Drug resistance and severe side effects limit current anticancer treatments.
- The coumarin scaffold is a versatile natural product motif with demonstrated antiproliferative activity.
Purpose of the Study:
- To review recent advances in the development of coumarin-containing hybrids as anticancer agents.
- To explore structure-activity relationships and mechanisms of action for these compounds.
- To highlight the potential of coumarin hybrids in overcoming cancer drug resistance.
Main Methods:
- Literature review of studies published between 2015 and 2019.
- Analysis of structure-activity relationships (SAR) of coumarin hybrids.
- Discussion of diverse antiproliferative mechanisms exhibited by coumarin derivatives.
Main Results:
- Coumarin hybrids demonstrate significant antiproliferative effects against various cancer types.
- Hybridization strategies can enhance efficacy and reduce toxicity compared to parent compounds.
- Emerging evidence supports coumarin hybrids as potential agents against multidrug-resistant cancers.
Conclusions:
- Coumarin-containing hybrids represent a promising class of novel anticancer agents.
- These hybrids offer potential for improved therapeutic interventions by addressing drug resistance and side effects.
- Further research into coumarin hybrids is warranted for their clinical application in cancer therapy.
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