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Efficient synthesis of Hsp90 inhibitor dimers as potential antitumor agents.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

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

doi

10.1016/j.bmc.2010.05.075

subject

Has Abstract

pub_date

2010-08-01 00:00:00

pages

5732-7

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00506-7

journal_volume

18

pub_type

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