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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.
- 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.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Novobiocin chemical synthesis
Novobiocin chemistry
Stereoisomerism
Structure-Activity Relationship
Antineoplastic Agents pharmacology
HSP90 Heat-Shock Proteins antagonists & inhibitors
Novobiocin pharmacology
Triazoles chemistry
Subjects
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