1301177-99-0Relevant 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.
scheme or table, 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.
