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

29 Scopus citations

Abstract

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
Volume18
Issue number9
DOIs
StatePublished - May 1 2008

Keywords

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

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