1301178-04-0Relevant articles and documents
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity
Zapf, Christoph W.,Bloom, Jonathan D.,McBean, Jamie L.,Dushin, Russell G.,Nittoli, Thomas,Ingalls, Charles,Sutherland, Alan G.,Sonye, John P.,Eid, Clark N.,Golas, Jennifer,Liu, Hao,Boschelli, Frank,Hu, Yongbo,Vogan, Erik,Levin, Jeremy I.
, p. 2278 - 2282 (2011/06/17)
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.
