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Updated: Jul 5, 2026

Optimizing Tubulin Yield from Porcine Brain Tissue
Published on: October 11, 2024
Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives
Ranganathan Balasubramanian1, Bhooma Raghavan, Jaeson C Steele
1Department of Medicinal Chemistry, 308 Harvard Street S.E., 8-101 Weaver-Densford Hall, University of Minnesota, Minneapolis, MN 55455-0353, USA.
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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