Abstract
The stereoselective preparation of several molecules containing structural fragments of the tetrahydrofuran and spiroacetal type is described. Their degree of cytotoxicity and their interactions with tubulin have been investigated. It has been confirmed that the tetrahydrofuran derivatives are cytotoxic but, in contrast to previous reports, it has been found that the cytoxicity is not due to interactions with the microtubule network. Furthermore, and also in contrast to a previous report on closely related compounds, the spiroacetal derivatives do show interactions with tubulin, even though the precise mechanism and the binding site still remain to be established.
Keywords: Tubulin, microtubules, cytoskeleton, microtubule-disrupting compounds, apoptosis, cytotoxicity, antitumoral drugs, anticancer therapy, bioactive structural fragments, tetrahydrofuran derivatives, spiroacetals
Current Medicinal Chemistry
Title:Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives
Volume: 20 Issue: 9
Author(s): M. Carda, J. Murga, J. Panos, C. A. Angulo-Pachon, J. Garcia-Pla, S. Diaz-Oltra, J. A. Marco, C. Trigili, M. Redondo-Horcajo, J. F. Diaz and I. Barasoain
Affiliation:
Keywords: Tubulin, microtubules, cytoskeleton, microtubule-disrupting compounds, apoptosis, cytotoxicity, antitumoral drugs, anticancer therapy, bioactive structural fragments, tetrahydrofuran derivatives, spiroacetals
Abstract: The stereoselective preparation of several molecules containing structural fragments of the tetrahydrofuran and spiroacetal type is described. Their degree of cytotoxicity and their interactions with tubulin have been investigated. It has been confirmed that the tetrahydrofuran derivatives are cytotoxic but, in contrast to previous reports, it has been found that the cytoxicity is not due to interactions with the microtubule network. Furthermore, and also in contrast to a previous report on closely related compounds, the spiroacetal derivatives do show interactions with tubulin, even though the precise mechanism and the binding site still remain to be established.
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Carda M., Murga J., Panos J., A. Angulo-Pachon C., Garcia-Pla J., Diaz-Oltra S., A. Marco J., Trigili C., Redondo-Horcajo M., F. Diaz J. and Barasoain I., Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives, Current Medicinal Chemistry 2013; 20 (9) . https://dx.doi.org/10.2174/0929867311320090006
DOI https://dx.doi.org/10.2174/0929867311320090006 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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