The invention relates to 1,3-Tellurazolidine-4-carboxylic acid, a stable cyclic telluro-amino acid synthesized from tellurocystine. This novel compound exhibits significant anticancer activity, particularly against breast cancer cell line MCF-7, with enhanced apoptotic effects and minimal toxicity to normal cells. The innovative synthesis method uses diiodomethane for efficient cyclization, avoiding decomposition issues. The compound’s high stability, biocompatibility, and broad therapeutic potential make it a versatile candidate for treating various diseases, including cancer, microbial infections, inflammation, and viral diseases. Additionally, the invention encompasses pharmaceutical compositions and various dosage forms, ensuring flexible and effective administration for diverse medical applications.
Despite advancements in organotellurium compounds, several challenges limit their therapeutic potential:
- Stability Issues: Tellurium-containing compounds, like tellurocysteine (TeCys), are unstable and prone to oxidation, restricting their therapeutic use.
- Bioavailability and Incorporation: Effective bioincorporation of tellurium into proteins has not been achieved through direct synthetic methods.
- Size and Accessibility: Larger compounds, such as HO-EGX-CY-Te-EGX-CY-OH, have difficulty reaching target sites within biological systems.
- Lack of Novel Compounds: Current research focuses on composites and nanoparticles but lacks novel organic tellurium compounds that can act as standalone drugs.
The technology gives the method to synthesise 1,3-Tellurazoldine-4-carboxylic acid, which has the following advantages:
- Stability and Biocompatibility: It is stable at room temperature and maintains high biocompatibility, with over 80% cell viability in normal cells, ensuring minimal toxicity.
- Significant Anticancer Activity: The compound shows potent anticancer effects, and enhanced apoptotic activity by arresting the sub G1 phase.
- Novel and Efficient Synthesis utilising diiodomethane for cyclisation, avoiding decomposition issues and enabling large-scale production.
- Versatile Pharmaceutical Applications: The compound can be formulated into various dosage forms, including capsules, tablets, and injections, allowing flexible administration methods.
- Broad Therapeutic Potential: Beyond anticancer properties, the compound has potential applications as an antimicrobial, anti-inflammatory, antiviral, and immunomodulating agent, making it a good candidate for multiple therapeutic uses.
A lab-scale prototype of 1,3-Tellurazolidine-4-Carboxylic Acid was synthesized using diiodomethane-mediated cyclization. The compound was characterized and tested in vitro against MCF-7 breast cancer cells, showing a potent IC50 of 7.29μg/ml and >80% viability in normal cells, confirming its stability, biocompatibility, and anticancer potential.
The compound showed an IC50 value of 7.29±0.27 μg/ml against breast cancer cell line MCF-7, demonstrating potent anticancer activity.
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- With its potent anticancer activity, the compound offers a promising new treatment option for cancer patients, particularly those with resistant forms of cancer like breast cancer. This could improve survival rates and quality of life for many patients.
- By providing new treatments for critical diseases, this technology can help reduce the global burden of illness, particularly in areas with limited access to advanced medical therapies.
- The novel, efficient, and scalable synthesis process allows for cost-effective production. This could reduce the overall cost of drug development and make new treatments more accessible to a broader population.
With its potent anticancer activity, the compound offers a promising new treatment option for cancer patients, particularly those with resistant forms of cancer like breast cancer. Beyond anticancer properties, the compound has potential applications as an antimicrobial, anti-inflammatory, antiviral, and immunomodulating agent, making it a versatile candidate for multiple therapeutic uses.
Geography of IP
Type of IP
202321008643
454497