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Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 11, 2011, Pages 3411-3416

Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity

(14) Zapf, Christoph W a Bloom, Jonathan D a McBean, Jamie L a Dushin, Russell G a Nittoli, Thomas a Otteng, Mercy a Ingalls, Charles a Golas, Jennifer M b Liu, Hao b Lucas, Judy b Boschelli, Frank b Hu, Yongbo c Vogan, Erik c Levin, Jeremy I a

a Discovery Medicinal Chemistry (United States)

b Oncology Research (United States)

c PFIZER INC (United States)

Author keywords

Buchwald Hartwig cyclization; Hsp90 inhibitors; Macrocycles; Ortho aminobenzamides; Tumor exposure

Indexed keywords

ANTINEOPLASTIC AGENT; GELDANAMYCIN; HEAT SHOCK PROTEIN 90 INHIBITOR; MACROCYCLIC LACTAM;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EXPOSURE; DRUG STRUCTURE; IC 50; IN VITRO STUDY; TUMOR CELL LINE;

ANIMALS; ANTHRANILIC ACIDS; ANTINEOPLASTIC AGENTS; BIOLOGICAL MARKERS; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; FLUORESCENT DYES; HSP90 HEAT-SHOCK PROTEINS; HUMANS; INHIBITORY CONCENTRATION 50; LACTAMS, MACROCYCLIC; MODELS, MOLECULAR; MOLECULAR STRUCTURE;

EID: 79956157504 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2011.03.112 Document Type: Article

Times cited : (17)

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