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3qtf

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3qtf, resolution 1.57Å ()
Ligands: ,
Gene: HSP90A, HSP90AA1, HSPC1, HSPCA (Homo sapiens)


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity

Publication Abstract from PubMed

A novel series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. A basic nitrogen within the tether linking the aniline nitrogen atom to a tetrahydroindolone moiety allowed access to compounds with good physical properties. Important structure-activity relationship information was obtained from this series which led to the discovery of a soluble and stable compound which is potent in an Hsp90 binding and cell-proliferation assay.

Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity., Zapf CW, Bloom JD, McBean JL, Dushin RG, Nittoli T, Ingalls C, Sutherland AG, Sonye JP, Eid CN, Golas J, Liu H, Boschelli F, Hu Y, Vogan E, Levin JI, Bioorg Med Chem Lett. 2011 Apr 15;21(8):2278-82. Epub 2011 Feb 28. PMID:21420297

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

3qtf is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Zapf CW, Bloom JD, McBean JL, Dushin RG, Nittoli T, Ingalls C, Sutherland AG, Sonye JP, Eid CN, Golas J, Liu H, Boschelli F, Hu Y, Vogan E, Levin JI. Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2278-82. Epub 2011 Feb 28. PMID:21420297 doi:10.1016/j.bmcl.2011.02.101

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