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Literature DB >> 15548050

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

Abstract

A chimera composed of the natural products radicicol and geldanamycin has been prepared through an amide linkage connecting the resorcinol moiety of radicicol to the quinone ring of geldanamycin. The inhibitory activity of these compounds was determined by their ability to inhibit Hsp90's inherent ATPase activity along with degradation of the Hsp90 client protein, HER-2 in MCF-7 breast cancer cells. [reaction: see text]

Entities: Chemical Disease Gene

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Year: 2004 PMID： 15548050 DOI： 10.1021/ol048266o

Source DB: PubMed Journal: Org Lett ISSN： 1523-7052 Impact factor: 6.005

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Cited

21 in total

1. Inhibition of heat-shock protein 90 reduces Ebola virus replication.

Authors: Darci R Smith; Sarah McCarthy; Andrew Chrovian; Gene Olinger; Andrea Stossel; Thomas W Geisbert; Lisa E Hensley; John H Connor
Journal: Antiviral Res Date: 2010-05-07 Impact factor: 5.970

2. Development of a Grp94 inhibitor.

Authors: Adam S Duerfeldt; Laura B Peterson; Jason C Maynard; Chun Leung Ng; Davide Eletto; Olga Ostrovsky; Heather E Shinogle; David S Moore; Yair Argon; Christopher V Nicchitta; Brian S J Blagg
Journal: J Am Chem Soc Date: 2012-05-29 Impact factor: 15.419

3. Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.

Authors: Hardik J Patel; Pallav D Patel; Stefan O Ochiana; Pengrong Yan; Weilin Sun; Maulik R Patel; Smit K Shah; Elisa Tramentozzi; James Brooks; Alexander Bolaender; Liza Shrestha; Ralph Stephani; Paola Finotti; Cynthia Leifer; Zihai Li; Daniel T Gewirth; Tony Taldone; Gabriela Chiosis
Journal: J Med Chem Date: 2015-04-22 Impact factor: 7.446

4. Trifunctional High-Throughput Screen Identifies Promising Scaffold To Inhibit Grp94 and Treat Myocilin-Associated Glaucoma.

Authors: Dustin J E Huard; Vincent M Crowley; Yuhong Du; Ricardo A Cordova; Zheying Sun; Moya O Tomlin; Chad A Dickey; John Koren; Laura Blair; Haian Fu; Brian S J Blagg; Raquel L Lieberman
Journal: ACS Chem Biol Date: 2018-02-20 Impact factor: 5.100

9. Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding.

Authors: Nanette L S Que; Vincent M Crowley; Adam S Duerfeldt; Jinbo Zhao; Caitlin N Kent; Brian S J Blagg; Daniel T Gewirth
Journal: J Med Chem Date: 2018-03-20 Impact factor: 7.446

10. Synthesis and evaluation of radamide analogues, a chimera of radicicol and geldanamycin.

Authors: M Kyle Hadden; Brian S J Blagg
Journal: J Org Chem Date: 2009-07-03 Impact factor: 4.354

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

1. Inhibition of heat-shock protein 90 reduces Ebola virus replication.

2. Development of a Grp94 inhibitor.

3. Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.

4. Trifunctional High-Throughput Screen Identifies Promising Scaffold To Inhibit Grp94 and Treat Myocilin-Associated Glaucoma.

5. Synthesis of a versatile metacyclophane macrolactam.

6. Development of radamide analogs as Grp94 inhibitors.

7. A structurally simplified analogue of geldanamycin exhibits neuroprotective activity.

8. Structure of the yeast spliceosomal postcatalytic P complex.

9. Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding.

10. Synthesis and evaluation of radamide analogues, a chimera of radicicol and geldanamycin.