Azides derived from colchicine and their use in library synthesis: A practical entry to new bioactive derivatives of an old natural drug

Abstract

(Chemical Equation Presented) Arresting cancer: The well-known tubulin-binding agent colchicine was diversified through a click conjugation approach. The key azide, readily prepared from desacetylcolchicine by diazo transfer, was efficiently converted to various triazoles. Biological evaluation of these triazoles revealed their potential as anti-tumor agents for further development. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.