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Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives |
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| Authors: | Balasubramanian Ranganathan Raghavan Bhooma Steele Jaeson C Sackett Dan L Fecik Robert A |
| Institution: | aDepartment of Medicinal Chemistry, 308 Harvard Street S.E., 8-101 Weaver–Densford Hall, University of Minnesota, Minneapolis, MN 55455-0353, USA bLaboratory of Integrative and Medical Biophysics, National Institute of Child Health and Human Development, National Institutes of Health, 9 Memorial Drive, Building 9, Room 1E129, Bethesda, MD 20892-0924, 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 IC50 values similar to combretastatin A4 and the hemiasterlin analog HTI-286. |
| Keywords: | Tubulysin Tubulin Anticancer agents Cytotoxicity Natural products |
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