Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives

Ranganathan Balasubramanian, Bhooma Raghavan, Jaeson C. Steele, Dan L. Sackett, Robert A. Fecik

Research output: Contribution to journalArticlepeer-review

32 Scopus citations


A series of tubulysin analogs in which one of the stereogenic centers of tubuphenylalanine was eliminated were synthesized. All compounds were tested for antiproliferative activity towards ovarian cancer cells and for inhibition of tubulin polymerization. The dimethyl analogs were generally more active than the desmethyl analogs, and four analogs have tubulin polymerization IC50 values similar to combretastatin A4 and the hemiasterlin analog HTI-286.

Original languageEnglish (US)
Pages (from-to)2996-2999
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number9
StatePublished - May 1 2008

Bibliographical note

Funding Information:
This work was generously supported by the American Cancer Society, Grant RSG-05-105-01-CDD (to R.A.F.), and was supported in part by intramural funds from the National Institute of Child Health and Human Development, NIH. Funding for NMR instrumentation in the Department of Biochemistry, Molecular Biology, and Biophysics was provided by the University of Minnesota Medical School, NSF (BIR-961477), and the Minnesota Medical Foundation.

Copyright 2008 Elsevier B.V., All rights reserved.


  • Anticancer agents
  • Cytotoxicity
  • Natural products
  • Tubulin
  • Tubulysin


Dive into the research topics of 'Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives'. Together they form a unique fingerprint.

Cite this