Literature DB >> 22014546

Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors.

Bhaskar Reddy Kusuma1, Adam S Duerfeldt, Brian S J Blagg.   

Abstract

Novobiocin analogs lacking labile glycosidic ether have been designed, synthesized and evaluated for Hsp90 inhibitory activity. Replacement of the synthetically complex noviose sugar with simple aromatic side chains produced analogs that maintain moderate cytotoxic activity against MCF7 and SkBR3 breast cancer cell-lines. Rationale for the preparation of des-noviose novobiocin analogs in addition to their synthesis and biological evaluation are presented herein. Copyright Â
© 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22014546      PMCID： PMC3242434          DOI： 10.1016/j.bmcl.2011.09.073

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  34 in total

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Review 3.  Structure and mechanism of the Hsp90 molecular chaperone machinery.

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4.  A library of noviosylated coumarin analogues.

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5.  New novobiocin analogues as antiproliferative agents in breast cancer cells and potential inhibitors of heat shock protein 90.

Authors:  Gaëlle Le Bras; Christine Radanyi; Jean-François Peyrat; Jean-Daniel Brion; Mouâd Alami; Véronique Marsaud; Barbara Stella; Jack-Michel Renoir
Journal:  J Med Chem       Date:  2007-11-03       Impact factor: 7.446

6.  A non-toxic Hsp90 inhibitor protects neurons from Abeta-induced toxicity.

Authors:  Sabah Ansar; Joseph A Burlison; M Kyle Hadden; Xiao Ming Yu; Kelly E Desino; Jennifer Bean; Len Neckers; Ken L Audus; Mary L Michaelis; Brian S J Blagg
Journal:  Bioorg Med Chem Lett       Date:  2007-01-17       Impact factor: 2.823

7.  Rational design of an aryl-C-glycoside catalyst from a natural product O-glycosyltransferase.

Authors:  Johannes Härle; Stefan Günther; Benjamin Lauinger; Monika Weber; Bernd Kammerer; David L Zechel; Andriy Luzhetskyy; Andreas Bechthold
Journal:  Chem Biol       Date:  2011-04-22

8.  Tosylcyclonovobiocic acids promote cleavage of the hsp90-associated cochaperone p23.

Authors:  Christine Radanyi; Gaëlle Le Bras; Céline Bouclier; Samir Messaoudi; Jean-François Peyrat; Jean-Daniel Brion; Mouâd Alami; Jack-Michel Renoir
Journal:  Biochem Biophys Res Commun       Date:  2008-12-30       Impact factor: 3.575

9.  KU135, a novel novobiocin-derived C-terminal inhibitor of the 90-kDa heat shock protein, exerts potent antiproliferative effects in human leukemic cells.

Authors:  Shary N Shelton; Mary E Shawgo; Shawna B Matthews; Yuanming Lu; Alison C Donnelly; Kristen Szabla; Mehmet Tanol; George A Vielhauer; Roger A Rajewski; Robert L Matts; Brian S J Blagg; John D Robertson
Journal:  Mol Pharmacol       Date:  2009-09-09       Impact factor: 4.436

10.  Novobiocin: redesigning a DNA gyrase inhibitor for selective inhibition of hsp90.

Authors:  Joseph A Burlison; Len Neckers; Andrew B Smith; Anthony Maxwell; Brian S J Blagg
Journal:  J Am Chem Soc       Date:  2006-12-06       Impact factor: 15.419
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  6 in total

1.  Alternative approaches to Hsp90 modulation for the treatment of cancer.

Authors:  Jessica A Hall; Leah K Forsberg; Brian S J Blagg
Journal:  Future Med Chem       Date:  2014-09       Impact factor: 3.808

2.  Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors.

Authors:  Takrima Sadikot; Megan Swink; Jeffery D Eskew; Douglas Brown; Huiping Zhao; Bhaskar R Kusuma; Roger A Rajewski; Brian S J Blagg; Robert L Matts; Jeffrey M Holzbeierlein; George A Vielhauer
Journal:  Assay Drug Dev Technol       Date:  2013-10-15       Impact factor: 1.738

3.  Synthesis and biological evaluation of coumarin replacements of novobiocin as Hsp90 inhibitors.

Authors:  Bhaskar Reddy Kusuma; Anuj Khandelwal; Wen Gu; Douglas Brown; Weiya Liu; George Vielhauer; Jeffrey Holzbeierlein; Brian S J Blagg
Journal:  Bioorg Med Chem       Date:  2014-01-03       Impact factor: 3.641

4.  Novobiocin Analogues That Inhibit the MAPK Pathway.

Authors:  Jessica A Hall; Sahithi Seedarala; Huiping Zhao; Gaurav Garg; Suman Ghosh; Brian S J Blagg
Journal:  J Med Chem       Date:  2016-01-27       Impact factor: 7.446

5.  KU-32, a novel drug for diabetic neuropathy, is safe for human islets and improves in vitro insulin secretion and viability.

Authors:  Kevin Farmer; S Janette Williams; Lesya Novikova; Karthik Ramachandran; Sonia Rawal; Brian S J Blagg; Rick Dobrowsky; Lisa Stehno-Bittel
Journal:  Exp Diabetes Res       Date:  2012-11-01

6.  A novel function of novobiocin: disrupting the interaction of HIF 1α and p300/CBP through direct binding to the HIF1α C-terminal activation domain.

Authors:  Donglu Wu; Rui Zhang; Rui Zhao; Guang Chen; Yong Cai; Jingji Jin
Journal:  PLoS One       Date:  2013-05-06       Impact factor: 3.240
  6 in total

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