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

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 manuf...

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Autores principales: Alcolea, Verónica, Garnica, Pablo, Palop, Juan A., Sanmartín, Carmen, González-Peñas, Elena, Durán, Adrián, Lizarraga, Elena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152329/
https://www.ncbi.nlm.nih.gov/pubmed/28786948
http://dx.doi.org/10.3390/molecules22081314
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author Alcolea, Verónica
Garnica, Pablo
Palop, Juan A.
Sanmartín, Carmen
González-Peñas, Elena
Durán, Adrián
Lizarraga, Elena
author_facet Alcolea, Verónica
Garnica, Pablo
Palop, Juan A.
Sanmartín, Carmen
González-Peñas, Elena
Durán, Adrián
Lizarraga, Elena
author_sort Alcolea, Verónica
collection PubMed
description 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.
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spelling pubmed-61523292018-11-13 Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation Alcolea, Verónica Garnica, Pablo Palop, Juan A. Sanmartín, Carmen González-Peñas, Elena Durán, Adrián Lizarraga, Elena Molecules Article 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. MDPI 2017-08-08 /pmc/articles/PMC6152329/ /pubmed/28786948 http://dx.doi.org/10.3390/molecules22081314 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Alcolea, Verónica
Garnica, Pablo
Palop, Juan A.
Sanmartín, Carmen
González-Peñas, Elena
Durán, Adrián
Lizarraga, Elena
Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title_full Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title_fullStr Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title_full_unstemmed Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title_short Antitumoural Sulphur and Selenium Heteroaryl Compounds: Thermal Characterization and Stability Evaluation
title_sort antitumoural sulphur and selenium heteroaryl compounds: thermal characterization and stability evaluation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152329/
https://www.ncbi.nlm.nih.gov/pubmed/28786948
http://dx.doi.org/10.3390/molecules22081314
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