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J Med Chem. 2009 Jan 22;52(2):238-40. doi: 10.1021/jm8013579.

Total synthesis and biological evaluation of tubulysin U, tubulysin V, and their analogues.

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  • 1Department of Medicinal Chemistry, 308 Harvard Street SE, 8-101 Weaver-Densford Hall, University of Minnesota, Minneapolis, Minnesota 55455-0353, USA.

Abstract

A stereoselective total synthesis of the cytotoxic natural products tubulysin U, tubulysin V, and its unnatural epimer epi-tubulysin V, is reported. Simplified analogues containing N,N-dimethyl-D-alanine as a replacement for the N-terminal N-Me-pipecolinic acid residue of the tubulysins are also disclosed. Biological evaluation of these natural products and analogues provided key information with regard to structural and stereochemical requirements for antiproliferative activity and tubulin polymerization inhibition.

PMID:
19102699
[PubMed - indexed for MEDLINE]
PMCID:
PMC4183140
Free PMC Article
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