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Azides Derived from Colchicine and their Use in Library Synthesis: a Practical Entry to New Bioactive Derivatives of an Old Natural Drug
Author(s) -
Nicolaus Norman,
Zapke Janet,
Riesterer Philipp,
Neudörfl JörgMartin,
Prokop Aram,
Oschkinat Hartmut,
Schmalz HansGünther
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000063
Subject(s) - diazo , colchicine , computer science , combinatorial chemistry , key (lock) , tubulin , chemistry , antimitotic agent , computational biology , biology , microtubule , organic chemistry , genetics , computer security , microbiology and biotechnology
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 antitumor agents for further development.