Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4602-4607

  Zapf, Christoph W ^a   Bloom, Jonathan D ^a   Li, Zhong ^a   Dushin, Russell G ^a   Nittoli, Thomas ^a   Otteng, Mercy ^a   Nikitenko, Antonia ^a   Golas, Jennifer M ^a   Liu, Hao ^a   Lucas, Judy ^a   Boschelli, Frank ^a   Vogan, Erik ^a   Olland, Andrea ^a   Johnson, Mark ^a   Levin, Jeremy I ^a  

^a PFIZER INC   (United States)

Author keywords

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

Indexed keywords

ALVESPIMYCIN; ANTINEOPLASTIC AGENT; GELDANAMYCIN; HEAT SHOCK PROTEIN 90 INHIBITOR; ISOXAZOLE; SNX 5422; TANESPIMYCIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL PROLIFERATION; CELL STRAIN HCT116; DRUG BINDING; DRUG POTENCY; GROWTH INHIBITION; HUMAN; HUMAN CELL; IC 50; LUNG CANCER; MAXIMUM PLASMA CONCENTRATION; MICROSOME; MOUSE; NONHUMAN; TIME TO MAXIMUM PLASMA CONCENTRATION; TUMOR VOLUME; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; BENZAMIDES; BINDING SITES; BIOLOGICAL MARKERS; DRUG EVALUATION, PRECLINICAL; HSP90 HEAT-SHOCK PROTEINS; HUMANS; LUNG NEOPLASMS; MACROCYCLIC COMPOUNDS; MICE; MICE, NUDE; MICROSOMES, LIVER; PROTEIN STRUCTURE, TERTIARY; RATS; TRANSPLANTATION, HETEROLOGOUS;

EID: 79960342165     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.102     Document Type: Article

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33. The structure has been assigned PDB ID code 3RKZ.