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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.

Original publication

DOI

10.3390/molecules22081314

Type

Journal article

Journal

Molecules

Publication Date

08/08/2017

Volume

22

Keywords

HPLC, X-ray diffraction, activity, differential scanning calorimetry, polymorphism, stability, thermal analysis, thermogravimetry, Antineoplastic Agents, Calorimetry, Differential Scanning, Cell Line, Tumor, Cell Survival, Chromatography, High Pressure Liquid, Drug Stability, Humans, Magnetic Resonance Spectroscopy, Molecular Structure, Selenium, Sensitivity and Specificity, Stress, Physiological, Sulfur, Thermogravimetry, X-Ray Diffraction