2. Academic Validation
  3. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design

Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design

  • J Med Chem. 2009 Mar 26;52(6):1510-3. doi: 10.1021/jm801627a.
Douglas S Williamson 1,  Jenifer Borgognoni,  Alexandra Clay,  Zoe Daniels,  Pawel Dokurno,  Martin J Drysdale,  Nicolas Foloppe,  Geraint L Francis,  Christopher J Graham,  Rob Howes,  Alba T Macias,  James B Murray,  Rachel Parsons,  Terry Shaw,  Allan E Surgenor,  Lindsey Terry,  Yikang Wang,  Mike Wood,  Andrew J Massey
Affiliations

Affiliation

  • 1 Vernalis (R&D) Ltd., Granta Park, Great Abington, Cambridge CB21 6GB, United Kingdom. d.williamson@vernalis.com
PMID: 19256508 DOI: 10.1021/jm801627a
Abstract

The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highly selective over HSP90, and some displayed potency against HCT116 cells. Exposure of compound 12 to HCT116 cells caused significant reduction in cellular levels of Raf-1 and Her2 at concentrations similar to that which caused cell growth arrest.

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