Back to Search Start Over

Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues.

Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues.

Authors :
Peterson LB
Blagg BS
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Jul 01; Vol. 20 (13), pp. 3957-60. Date of Electronic Publication: 2010 May 06.
Publication Year :
2010

Abstract

A series of triazole-containing novobiocin analogues has been designed, synthesized and their inhibitory activity determined. These compounds contain a triazole ring in lieu of the amide moiety present in the natural product. The anti-proliferative effects of these compounds were evaluated against two breast cancer cell lines (SKBr-3 and MCF-7), and manifested activities similar to their amide-containing counterparts. In addition, Hsp90-dependent client protein degradation was observed via Western blot analyses, supporting a common mode of Hsp90 inhibition for both structural classes.<br /> (2010 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
20
Issue :
13
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
20570149
Full Text :
https://doi.org/10.1016/j.bmcl.2010.04.140