2. Academic Validation
  3. Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives

Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2996-9. doi: 10.1016/j.bmcl.2008.03.046.
Ranganathan Balasubramanian 1,  Bhooma Raghavan,  Jaeson C Steele,  Dan L Sackett,  Robert A Fecik
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, 308 Harvard Street S.E., 8-101 Weaver-Densford Hall, University of Minnesota, Minneapolis, MN 55455-0353, USA.
PMID: 18411048 DOI: 10.1016/j.bmcl.2008.03.046
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 IC(50) values similar to combretastatin A4 and the hemiasterlin analog HTI-286.

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