Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents

H Sekiguchi, K Muranaka, A Osada, S Ichikawa…

Index: Sekiguchi, Hironori; Muranaka, Kazuhiro; Osada, Akiko; Ichikawa, Satoshi; Matsuda, Akira Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 15 p. 5732 - 5737

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Citation Number: 5

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 ...