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

Ranganathan Balasubramanian, Bhooma Raghavan, Adrian Begaye, Dan L. Sackett, Robert A. Fecik

Research output: Contribution to journalArticlepeer-review

47 Scopus citations

Abstract

A stereoselective total synthesis of the cytotoxic natural products tubulysin U, tubulysin V, and its unnatural epimer epitubulysin 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.

Original languageEnglish (US)
Pages (from-to)238-240
Number of pages3
JournalJournal of medicinal chemistry
Volume52
Issue number2
DOIs
StatePublished - Jan 22 2009

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