The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 14, 2005, Pages 3338-3343

  Cheung, Kwai Ming J ^a   Matthews, Thomas P ^a   James, Karen ^a   Rowlands, Martin G ^a   Boxall, Katherine J ^a   Sharp, Swee Y ^a   Maloney, Alison ^a   Roe, S Mark ^b   Prodromou, Chrisostomos ^b   Pearl, Laurence H ^b   Aherne, G Wynne ^a   McDonald, Edward ^a   Workman, Paul ^a  

^a IMPERIAL CANCER RESEARCH FUND   (United Kingdom)

^b INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

Cancer; Hsp90 inhibitors; Protein crystal structure; Pyrazole; Resorcinol

Indexed keywords

CCT 018159; CCT 069965; CCT 072439; CCT 072440; CCT 072442; CCT 072453; CCT 072454; CCT 072457; CCT 073657; CCT 073667; CCT 074897; CCT 074898; CCT 075450; ENZYME INHIBITOR; GELDANAMYCIN; HEAT SHOCK PROTEIN 90; PROTEIN INHIBITOR; PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CANCER CELL CULTURE; COLON CANCER; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATASES; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HETEROCYCLIC COMPOUNDS, 2-RING; HSP90 HEAT-SHOCK PROTEINS; HUMANS; HYDROGEN BONDING; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PROTEIN CONFORMATION; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; YEASTS;

EID: 20644448390     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.05.046     Document Type: Article

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