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

Cardá, Miguel; Murga, Juan; Paños, Julián Toledo; García-Pla, Jorge; Díaz‐Oltra, Santiago; Marco, J. Alberto; Trigili, Chiara; Redondo‐Horcajo, Mariano; Díaz, J. Fernando; Barasoaín, Isabel

doi:10.2174/0929867311320090006

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Cited by 6 publications

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Design and Synthesis of Pironetin Analogue/Combretastatin A‐4 Hybrids and Evaluation of Their Cytotoxic Activity

Torijano-Gutiérrez¹,

Vilanova²,

Díaz‐Oltra³

et al. 2014

Eur J Org Chem

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We here describe the preparation of a series of hybrid molecules containing a combretastatin A-4 moiety and a pironetin analogue fragment. The cytotoxic activities of these compounds have been measured. Relations between structure and cytotoxicity are discussed. Some of the tested compounds showed cytotoxicity values of the same order of magnitude as the parental molecules, combretastatin A-4 and pironetin, and were less toxic than the latter for normal cells.  The normal vs. tumoral cytotoxicity ratio of some of the tested compounds are higher than in the case of the parental molecules, that is, they are safer than the latter compounds.

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