Tubulin-polymerization inhibitors derived from thalidomide

  • Bioorg Med Chem Lett. 2005 Jan 17;15(2):321-5. doi: 10.1016/j.bmcl.2004.10.072.
Shunsuke Inatsuki  1 ,  Tomomi Noguchi ,  Hiroyuki Miyachi ,  Sawako Oda ,  Toyotaka Iguchi ,  Masahiro Kizaki ,  Yuichi Hashimoto ,  Hisayoshi Kobayashi
Affiliations
  • 1. Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
PMID: 15603947 DOI: 10.1016/j.bmcl.2004.10.072
Abstract

2-(2,6-Diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione (5HPP-33), which was obtained during our previous structural development studies on thalidomide, was revealed to possess potent tubulin-polymerization-inhibiting activity, comparable to that of the known tubulin-polymerization inhibitors, rhizoxin and colchicine. A major metabolite of thalidomide, 5-hydroxythalidomide, which possesses a hydroxyl group at the position corresponding to that of 5HPP-33, also showed moderate inhibitory activity.

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