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Bioorg Med Chem Lett. 2004 Jan 19;14(2):325-8.

Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.

Author information

1
RiboTargets Ltd, Granta Park, CB1 6GB, Cambridge, UK. b.dymock@ribotargets.com

Abstract

Multiple co-crystal structures of an adenine-based series of inhibitors bound to the molecular chaperone Hsp90 have been determined. These structures explain the observed SAR for previously described compounds and new compounds, which possess up to 8-fold improved potency against the isolated enzyme. Anti-tumour cell potency and mechanism of action data is also described for the most potent compounds. These data should enable the design of more potent Hsp90 inhibitors.

PMID:
14698151
DOI:
10.1016/j.bmcl.2003.11.011
[Indexed for MEDLINE]

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