| Novel structural insights for imidoselenocarbamates with antitumoral activity related to their ability to generate methylselenol. | |
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MedLine Citation:
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PMID: 22863528 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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In the search for molecules with potential antiangiogenic activity we found that several imidoselenocarbamate derivatives, which have pro-apoptotic and antiproliferative activities, under hypoxic conditions release methylselenol, a volatile and highly reactive gas that was considered to be responsible for the observed biological activity. The kinetic for the liberation of methylselenol is highly dependent on the nature of the overall structure and correlate with their proven pro-apoptotic activity in lung cancer cell line H157. The preliminary structure-activity relationships allow us to select as the basic structural element a scaffold constructed with an imidoselenocarbamate fragment decorated with a methyl residue on the Se central atom and two heteroaromatic lateral rings. These imidoselenocarbamate derivatives may be of interest both for their antitumoral activities and because they have a structure that can be considered as a template for the design of new derivatives with apoptotic activity. This activity is related to the controlled delivery of methylselenol and makes this an interesting approach to develop new antitumoral agents. |
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Authors:
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María Font; Alicia Zuazo; Elena Ansó; Daniel Plano; Carmen Sanmartín; Juan-Antonio Palop; Juan-José Martínez-Irujo |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-7-15 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: - ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2012 Jul |
Date Detail:
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Created Date: 2012-8-6 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012 Elsevier Ltd. All rights reserved. |
Affiliation:
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Sección de Modelización Molecular, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Irunlarrea 1, E-31008 Pamplona, Spain. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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