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New C(4)‐Functionalized Colchicine Derivatives by a Versatile Multicomponent Electrophilic Aromatic Substitution
Authors:Nicolas Bensel  David Lagnoux  Verena Niggli  Markus Wartmann  Jean‐Louis Reymond
Abstract:Electrophilic alkylation of colchicine at C(4) was accomplished by a multicomponent aromatic electrophilic substitution reaction with electrophilic aldehydes and carboxylic acids or amides in H2SO4. A series of new derivatives were obtained and evaluated for their antiproliferative effect towards various tumor cell lines, and their stimulatory effect on the development of polarity in human neutrophils.
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