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.
