Solution-phase parallel synthesis and biological evaluation of combretatriazoles

…, E Del Grosso, A Massarotti, G Sorba…

Index: Pagliai, Francesca; Pirali, Tracey; Del Grosso, Erika; Di Brisco, Riccardo; Tron, Gian Cesare; Sorba, Giovanni; Genazzani, Armando A. Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 467 - 470

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Citation Number: 37

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 α-keto phosphorus ylids, which is known to regioselectively generate the 1, 5- ...