Development of tubulin-polymerization inhibitors based on the thalidomide skeleton |
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| Authors: | Aoyama Hiroshi Noguchi Tomomi Misawa Takashi Nakamura Takanori Miyachi Hiroyuki Hashimoto Yuichi Kobayashi Hisayoshi |
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| Affiliation: | Institute of Molecular & Cellular Biosciences, The University of Tokyo, Bunkyo-ku, Tokyo, Japan. aoyama@iam.u-tokyo.ac.jp |
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| Abstract: | We synthesized a series of compounds based on the potent tubulin-polymerization inhibitor 5-hydroxy-2-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione [5HPP-33 (3)], which is structurally derived from thalidomide (1), and investigated their inhibitory effects on tubulin polymerization. Direct interaction between 5HPP-33 (3) and alpha,beta-tubulin heterodimer protein was demonstrated by means of a surface plasmon resonance study. |
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