2. Academic Validation
  3. Synthesis, biological activity and tubulin binding poses of 1-deoxy-9-(R)-dihydrotaxane analogs

Synthesis, biological activity and tubulin binding poses of 1-deoxy-9-(R)-dihydrotaxane analogs

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1148-51. doi: 10.1016/j.bmcl.2008.12.091.
Tian-Hai Yuan 1,  Yi Jiang,  Xiao-Hong Wang,  Dian-Long Wang,  Abhijit Bannerjee,  Susan Bane,  James P Snyder,  Hai-Xia Lin
Affiliations

Affiliation

  • 1 Department of Chemistry, Shanghai University, Shanghai 200444, China.
PMID: 19136258 DOI: 10.1016/j.bmcl.2008.12.091
Abstract

1-Deoxy-9alpha-dihydrotaxane analogs 9 and 10 were semi-synthesized from 1-deoxybaccatin VI, isolated from Taxus mairei, and tested for cytotoxic activity. Taxane 9 is 10-fold less cytotoxic than paclitaxel, while 10 is equally active. In the tubulin polymerization assay (ED(50) values), 10 is 4-fold less effective than paclitaxel, but 3-fold superior to 9. These observations can be explained by analysis of the corresponding taxane/beta-tubulin complexes.

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