Journal
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2011, Issue 16, Pages 3050-3059Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201100155
Keywords
Natural products; Antitumor agents; Synthesis design; Myxobacteria; Tubulysins
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Funding
- Deutsche Forschungsgemeinschaft (DFG) [FOR 1406, Ka 880/10-1]
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The syntheses of new tubulysin analogues are described, in which the central amino acid, tubuvaline, is replaced by the rather simple building blocks phenyltubuvaline and phenoxytubuvaline. These analogues can be obtained in only two to three steps from easily accessible starting materials. Although the new derivatives are less active than the tubulysins, their activities towards U-2 OS tumor cells are still in the nanomolar range.
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