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Syntheses and Evaluation of Simplified Pretubulysin Analogues
Author(s) -
Burkhart Jens L.,
Müller Rolf,
Kazmaier Uli
Publication year - 2011
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201100155
Subject(s) - chemistry , combinatorial chemistry , stereochemistry , amino acid , biochemistry
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.