Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90

Journal of Medicinal Chemistry

Volumn 49, Issue 15, 2006, Pages 4606-4615

  Ge, Jie ^a   Normant, Emmanuel ^a   Porter, James R ^a   Ali, Janid A ^a   Dembski, Marlene S ^a   Gao, Yun ^a   Georges, Asimina T ^a   Grenier, Louis ^a   Pak, Roger H ^a   Patterson, Jon ^a   Sydor, Jens R ^a   Tibbitts, Thomas T ^a   Tong, Jeffrey K ^a   Adams, Julian ^a   Palombella, Vito J ^a  

^a Infinity Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

17 ALLYLAMINO 17 DEMETHOXYGELDANAMYCIN; 17 ALLYLAMINO 17 DEMETHOXYGELDANAMYCIN HYDROQUINONE; DRUG METABOLITE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; GLUCOSE REGULATED PROTEIN 94; HEAT SHOCK PROTEIN 90; HYDROQUINONE DERIVATIVE; IPI 504; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BIOLOGICAL ACTIVITY; CANCER CELL; CANCER CELL CULTURE; CANCER INHIBITION; CANCER THERAPY; CELL ACTIVITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENDOPLASMIC RETICULUM; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; MOLECULAR MODEL; NONHUMAN; PROTEIN INDUCTION; PROTEIN SYNTHESIS REGULATION;

ANIMALS; ANTINEOPLASTIC AGENTS; BENZOQUINONES; BINDING, COMPETITIVE; CELL LINE, TUMOR; DOGS; DRUG SCREENING ASSAYS, ANTITUMOR; FLUORESCENCE POLARIZATION; HSP70 HEAT-SHOCK PROTEINS; HSP90 HEAT-SHOCK PROTEINS; HUMANS; HYDROQUINONES; LACTAMS, MACROCYCLIC; MEMBRANE PROTEINS; MODELS, MOLECULAR; PROTEIN ISOFORMS; RECEPTOR, ERBB-2; RIFABUTIN; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; WATER;

EID: 33746662241     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0603116     Document Type: Article

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68. 1/2, half-life; TBST, Tris-buffered saline containing 0.1% Tween 20; TLR, Toll-like receptors; Trap 1, tumor necrosis factor receptor-associated protein 1.