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Online ISSN: 1860-7187
March 22, 2010
VIP: Azides Derived from Colchicine and Their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug
Norman Nicolaus, Janet Zapke, Philipp Riesterer, Jörg-Martin Neudörfl, Aram Prokop, Hartmut Oschkinat, and Hans-Günther Schmalz*
The natural product colchicine is an established antimitotic drug that targets microtubule formation by selective tubulin binding. In this paper Schmalz and colleagues report their efficient semisynthetic access to a library of novel colchicinoids, along with some initial screening results. K. Barry Sharpless commented on the work as being "one of the best quick-connect triazole SARs I've seen yet." Indeed, the compounds identified are promising candidates for the development of new antiproliferative drugs.
Received February 15, 2010; published online March 12, 2010, DOI: 10.1002/cmdc.201000063.