Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents |
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Authors: | Hironori Sekiguchi Kazuhiro Muranaka Akiko Osada Satoshi Ichikawa Akira Matsuda |
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Institution: | 1. Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan;2. Discovery & Development Laboratory I, Hanno Research Center, Taiho Pharmaceutical Co., Ltd, 1-27 Misugidai, Hanno, Saitama 357, Japan |
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Abstract: | The PU-H58-dimers 13a–15b were efficiently synthesized and their biological properties were evaluated. The copper-catalyzed alkyne azide coupling was effective in simultaneously linking three components via a triazole formation to afford the target dimers. These synthesized dimers exhibited binding affinity to the N-terminal domain of Hsp90, cytotoxicity, and client degradation activity although these activities were comparative or weak comparable with that of the parent compound. |
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