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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives

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

Volume 20 , Issue 9 , 2013

Page: [1173 - 1182] Pages: 10

DOI: 10.2174/0929867311320090006

Price: $65


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

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