Literature DB >> 19896848

Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors.

Vinod D Jadhav1, Adam S Duerfeldt, Brian S J Blagg.   

Abstract

Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.

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Year:  2009        PMID： 19896848      PMCID： PMC2784232          DOI： 10.1016/j.bmcl.2009.10.091

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


  18 in total

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2.  Design, synthesis, and evaluation of a radicicol and geldanamycin chimera, radamide.

Authors:  Randell C Clevenger; Brian S J Blagg
Journal:  Org Lett       Date:  2004-11-25       Impact factor: 6.005

3.  Radester, a novel inhibitor of the Hsp90 protein folding machinery.

Authors:  Gang Shen; Brian S J Blagg
Journal:  Org Lett       Date:  2005-05-26       Impact factor: 6.005

4.  Design, synthesis, and structure--activity relationships for chimeric inhibitors of Hsp90.

Authors:  Gang Shen; Mingwen Wang; Timothy R Welch; Brian S J Blagg
Journal:  J Org Chem       Date:  2006-09-29       Impact factor: 4.354

5.  Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.

Authors:  S M Roe; C Prodromou; R O'Brien; J E Ladbury; P W Piper; L H Pearl
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Review 7.  Hsp90 inhibitors: small molecules that transform the Hsp90 protein folding machinery into a catalyst for protein degradation.

Authors:  Brian S J Blagg; Timothy D Kerr
Journal:  Med Res Rev       Date:  2006-05       Impact factor: 12.944

8.  The heat shock protein 90 antagonist novobiocin interacts with a previously unrecognized ATP-binding domain in the carboxyl terminus of the chaperone.

Authors:  M G Marcu; A Chadli; I Bouhouche; M Catelli; L M Neckers
Journal:  J Biol Chem       Date:  2000-11-24       Impact factor: 5.157

9.  A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors.

Authors:  Adeela Kamal; Lia Thao; John Sensintaffar; Lin Zhang; Marcus F Boehm; Lawrence C Fritz; Francis J Burrows
Journal:  Nature       Date:  2003-09-25       Impact factor: 49.962

10.  Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation.

Authors:  L Whitesell; E G Mimnaugh; B De Costa; C E Myers; L M Neckers
Journal:  Proc Natl Acad Sci U S A       Date:  1994-08-30       Impact factor: 11.205
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  1 in total

1.  Structural determination of three different series of compounds as Hsp90 inhibitors using 3D-QSAR modeling, molecular docking and molecular dynamics methods.

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Journal:  Int J Mol Sci       Date:  2011-01-30       Impact factor: 5.923
  1 in total

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