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  • Title: Solution-phase parallel synthesis and biological evaluation of combretatriazoles.
    Author: Cafici L, Pirali T, Condorelli F, Del Grosso E, Massarotti A, Sorba G, Canonico PL, Tron GC, Genazzani AA.
    Journal: J Comb Chem; 2008; 10(5):732-40. PubMed ID: 18681482.
    Abstract:
    Combretastatin A-4 is an antitumoral and antitubulin agent that is active only in its cis configuration. In the present manuscript, we have synthesized cis-locked combretastatins containing a triazole ring (combretatriazoles). To achieve this, we have developed a column chromatography-free parallel solution-phase synthesis that exploits the reaction between azides and alpha-keto phosphorus ylids, which is known to regioselectively generate the 1,5-disubstituted triazoles. The prepared compounds were screened as antitubulinic agents, allowing us to identify three new compounds with high potency, two of which show a new mechanism of action that induces cells to appear multinucleated and display a high number of mitotic spindles.
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