Beilstein Journal of Organic Chemistry p. 535 - 543 (2014)
Update date:2022-07-30
Topics:
Harmrolfs, Kirsten
Mancuso, Lena
Drung, Binia
Sasse, Florenz
Kirschning, Andreas
The preparation of alkyne-modified ansamitocins by mutasynthetic supplementation of Actinosynnema pretiosum mutants with alkyne-substituted aminobenzoic acids is described. This modification paved the way to introduce a thiol linker by Huisgen-type cycloaddition which can principally be utilized to create tumor targeting conjugates. In bioactivity tests, only those new ansamitocin derivatives showed strong antiproliferative activity that bear an ester side chain at C-3.
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