Tubulin-polymerization inhibitors derived from thalidomide |
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Authors: | Inatsuki Shunsuke Noguchi Tomomi Miyachi Hiroyuki Oda Sawako Iguchi Toyotaka Kizaki Masahiro Hashimoto Yuichi Kobayashi Hisayoshi |
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Institution: | Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. |
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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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