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Molecules 2017, 22(8), 1314; doi:10.3390/molecules22081314

Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation

1
Department of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain
2
Department of Chemistry, Faculty of Sciences, University of Navarra, Irunlarrea 1, 31008 Pamplona, Spain
Authors have contributed equally to this article.
*
Author to whom correspondence should be addressed.
Received: 29 June 2017 / Accepted: 4 August 2017 / Published: 8 August 2017
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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. View Full-Text
Keywords: thermal analysis; activity; stability; polymorphism; differential scanning calorimetry; thermogravimetry; X-ray diffraction; HPLC thermal analysis; activity; stability; polymorphism; differential scanning calorimetry; thermogravimetry; X-ray diffraction; HPLC
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Alcolea, V.; Garnica, P.; Palop, J.A.; Sanmartín, C.; González-Peñas, E.; Durán, A.; Lizarraga, E. Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation. Molecules 2017, 22, 1314.

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