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

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 8, 2011, Pages 2278-2282

  Zapf, Christoph W ^a   Bloom, Jonathan D ^a   McBean, Jamie L ^a   Dushin, Russell G ^a   Nittoli, Thomas ^a   Ingalls, Charles ^a   Sutherland, Alan G ^a   Sonye, John P ^a   Eid, Clark N ^a   Golas, Jennifer ^a   Liu, Hao ^a   Boschelli, Frank ^a   Hu, Yongbo ^a   Vogan, Erik ^a   Levin, Jeremy I ^a  

^a PFIZER INC   (United States)

Author keywords

Buchwald Hartwig cyclization; Chaperon inhibitors; Hsp90 inhibitors; Macrocycles; N terminal ATP binding site; ortho Aminobenzamides

Indexed keywords

2 AMINOBENZAMIDE; ANILINE; GELDANAMYCIN; HEAT SHOCK PROTEIN 90 INHIBITOR; INDOLE DERIVATIVE; MACROCYCLIC COMPOUND; NITROGEN;

ANIMAL CELL; ARTICLE; CELL PROLIFERATION; CYCLIZATION; DRUG DESIGN; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; HUMAN; HUMAN CELL; MICROSOME; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; BENZAMIDES; BINDING SITES; CELL LINE, TUMOR; CELL PROLIFERATION; COMPUTER SIMULATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HSP90 HEAT-SHOCK PROTEINS; HUMANS; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79953281151     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.101     Document Type: Article

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27. manuscript in preparation
28. The structure has been assigned PDB ID code 3QTF.