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Development of 2,4-Substituted Thiazoles as Dual Inhibitors of Inflammation and Breast-Cancer Progression
1Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology, Vellore, Tamil Nadu, India.
Abstract:
Breast cancer remains a major cause of cancer-related mortality worldwide, with chronic inflammation recognized as a key contributor to its initiation and progression. This study aimed to develop 2,4-substituted thiazoles with dual anti-inflammatory and anticancer potential. A series of 20 2,4-substituted thiazoles 3(a-t) was synthesized and evaluated for biological efficacy. Antioxidant screening revealed compound 3t showed strong inhibition (IC50 = 26.53 ± 0.16 µg/mL). Anti-inflammatory protein denaturation assays demonstrated significant inhibition by compounds 3p and 3r (IC50 = 6.50 ± 0.89 and 10.72 ± 4.36 µg/mL). Cytotoxicity screening against MCF-7 breast cancer cells showed 3r had higher antiproliferative potency (IC50 = 17.44 µg/mL) than 3p, confirmed by cell cycle analysis and dual fluorescent staining, indicating mild apoptosis and suppressed proliferation. In silico ADME, drug-likeness, and network pharmacology analyses supported favorable pharmacokinetic profiles and identified potential molecular targets. Molecular docking revealed strong binding interactions. Overall, compound 4-(2-(2-((1-benzyl-1H-indol-3-yl)methylene)hydrazinyl)thiazol-4-yl)benzonitrile (3r) emerges as a promising multifunctional lead, highlighting the potential of 2,4-substituted thiazoles scaffolds in targeting inflammation-associated breast cancer. The novelty of this work lies in demonstrating the dual efficacy of these hybrids in modulating inflammatory and proliferative pathways, guiding future mechanistic and in vivo investigations.
Insights
Researchers developed novel 2,4-substituted thiazoles targeting inflammation and breast cancer. Compound 3r showed potent anti-inflammatory and anticancer activity, acting as a promising lead for future drug development.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Chronic inflammation is a key factor in breast cancer initiation and progression.
- There is a need for novel therapeutic agents with dual anti-inflammatory and anticancer properties.
Purpose of the Study:
- To synthesize and evaluate 2,4-substituted thiazoles for combined anti-inflammatory and anticancer potential.
- To identify lead compounds for targeting inflammation-associated breast cancer.
Main Methods:
- Synthesis of 20 2,4-substituted thiazole derivatives (compounds 3a-t).
- In vitro evaluation of antioxidant, anti-inflammatory (protein denaturation), and cytotoxic (MCF-7 cells) activities.
- In silico analyses including ADME, drug-likeness, network pharmacology, and molecular docking.
Main Results:
- Compound 3t exhibited strong antioxidant activity (IC50 = 26.53 µg/mL).
- Compounds 3p and 3r demonstrated significant anti-inflammatory effects (IC50 = 6.50 and 10.72 µg/mL, respectively).
- Compound 3r showed superior antiproliferative potency against MCF-7 cells (IC50 = 17.44 µg/mL), inducing mild apoptosis and suppressing proliferation. In silico studies supported favorable pharmacokinetics and identified potential targets.
Conclusions:
- Compound 4-(2-(2-((1-benzyl-1H-indol-3-yl)methylene)hydrazinyl)thiazol-4-yl)benzonitrile (3r) is a promising multifunctional lead compound.
- The 2,4-substituted thiazole scaffold holds potential for developing novel therapeutics for inflammation-associated breast cancer.
- The study highlights the dual efficacy of these hybrid compounds in modulating inflammatory and proliferative pathways.
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