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Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
Verónica Alcolea1, Pablo Garnica2, Juan A Palop3
1Department of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain. valcolea@alumni.unav.es.
Abstract:
The physicochemical properties of a compound play a crucial role in the cancer development process. In this context, polymorphism can become an important obstacle for the pharmaceutical industry because it frequently leads to the loss of therapeutic effectiveness of some drugs. Stability under manufacturing conditions is also critical to ensure no undesired degradations or transformations occur. In this study, the thermal behaviour of 40 derivatives of a series of sulphur and selenium heteroaryl compounds with potential antitumoural activity were studied. In addition, the most promising cytotoxic derivatives were analysed by a combination of differential scanning calorimetry, X-ray diffraction and thermogravimetric techniques in order to investigate their polymorphism and thermal stability. Moreover, stability under acid, alkaline and oxidative media was tested. Degradation under stress conditions as well as the presence of polymorphism was found for the compounds VA6E and VA7J, which might present a hurdle to carrying on with formulation. On the contrary, these obstacles were not found for derivative VA4J.
Insights
Polymorphism and degradation in potential anticancer drugs pose formulation challenges. Derivative VA4J showed promising stability, unlike VA6E and VA7J, indicating its suitability for pharmaceutical development.
Area of Science:
- Medicinal Chemistry
- Materials Science
- Pharmaceutical Sciences
Background:
- Physicochemical properties, including polymorphism, critically influence drug efficacy and development.
- Polymorphism can lead to loss of therapeutic effectiveness and presents challenges for the pharmaceutical industry.
- Ensuring drug stability during manufacturing is vital to prevent degradation and unwanted transformations.
Purpose of the Study:
- To investigate the thermal behavior, polymorphism, and stability of sulfur and selenium heteroaryl compounds with potential antitumoral activity.
- To identify derivatives suitable for pharmaceutical formulation by assessing their stability under various stress conditions.
Main Methods:
- Differential scanning calorimetry (DSC)
- X-ray diffraction (XRD)
- Thermogravimetric analysis (TGA)
- Stability testing in acidic, alkaline, and oxidative media.
Main Results:
- Forty sulfur and selenium heteroaryl derivatives were analyzed for their thermal behavior.
- Compounds VA6E and VA7J exhibited degradation under stress conditions and showed polymorphism, posing formulation hurdles.
- Derivative VA4J demonstrated stability and lacked polymorphism, indicating its potential for pharmaceutical development.
Conclusions:
- The physicochemical properties, particularly polymorphism and stability, are critical for the pharmaceutical development of antitumoral agents.
- VA4J is a promising candidate for further formulation due to its favorable stability profile.
- VA6E and VA7J require further investigation or modification to overcome formulation challenges.
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