Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

Journal of Medicinal Chemistry

Volumn 58, Issue 24, 2015, Pages 9480-9497

  Zhou, Han Jie ^a   Wang, Jinhai ^a   Yao, Bing ^a   Wong, Steve ^a   Djakovic, Stevan ^a   Kumar, Brajesh ^a   Rice, Julie ^a   Valle, Eduardo ^a   Soriano, Ferdie ^a   Menon, Mary Kamala ^a   Madriaga, Antonett ^a   Kiss Von Soly, Szerenke ^a   Kumar, Abhinav ^a   Parlati, Francesco ^a   Yakes, F Michael ^a   Shawver, Laura ^a   Le Moigne, Ronan ^a   Anderson, Daniel J ^a   Rolfe, Mark ^a   Wustrow, David ^a  

^a Cleave Biosciences   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (BENZYLAMINO) 5H,7H,8H PYRANO[4,3 D]PYRIMIDIN 2 YL] 2 METHYL 1H INDOLE 4 CARBOXAMIDE; ACETALDOXIME; ALUMINUM LITHIUM HYDRIDE; ANTINEOPLASTIC AGENT; BORON TRIBROMIDE; BORONIC ACID DERIVATIVE; BROMINE DERIVATIVE; CASPASE 3; ENAMINE; GROWTH ARREST AND DNA DAMAGE INDUCIBLE PROTEIN 153; HYDROXYL GROUP; IMIDAZOLE; INDOLE DERIVATIVE; ISOCYANIC ACID DERIVATIVE; NITROGEN; PALLADIUM; PALLADIUM ACETATE; PROTEASOME; PROTEIN P53; PROTEIN P62; PROTEIN P97; PYRIMIDINE DERIVATIVE; PYRIMIDINONE DERIVATIVE; QUINAZOLINE DERIVATIVE; SODIUM AZIDE; TRIPHENYLPHOSPHINE; UBIQUITIN; UNCLASSIFIED DRUG; ADENOSINE TRIPHOSPHATASE; CB-5083; NUCLEAR PROTEIN; P97 ATPASE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; BROMINATION; CACO 2 CELL LINE; CANCER CELL; CANCER INHIBITION; CARBOXYLATION; CATALYSIS; CATALYST; CELL DEATH; CELL VIABILITY; CHEMICAL STRUCTURE; CONTROLLED STUDY; CRYSTAL STRUCTURE; CYCLIZATION; DEBROMINATION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; ENDOPLASMIC RETICULUM ASSOCIATED DEGRADATION; ENDOPLASMIC RETICULUM STRESS; ENZYME ACTIVATION; ENZYME INHIBITION; HEMATOLOGIC MALIGNANCY; HUMAN; HUMAN CELL; HYDROGEN BOND; HYDROLYSIS; IC50; IN VITRO STUDY; IN VIVO STUDY; LUNG CANCER CELL LINE; METABOLIC STABILITY; MOUSE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; RAT; SIGNAL TRANSDUCTION; SOLID TUMOR; SUZUKI REACTION; SYNTHESIS; UNFOLDED PROTEIN RESPONSE; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; CANCER TRANSPLANTATION; CHEMISTRY; DRUG SCREENING; FEMALE; METABOLISM; MOLECULAR DOCKING; NUDE MOUSE; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE; XENOGRAFT;

ADENOSINE TRIPHOSPHATASES; ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HETEROGRAFTS; HUMANS; INDOLES; MICE, NUDE; MOLECULAR DOCKING SIMULATION; NEOPLASM TRANSPLANTATION; NUCLEAR PROTEINS; PROTEASOME ENDOPEPTIDASE COMPLEX; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; UBIQUITIN; UNFOLDED PROTEIN RESPONSE;

EID: 84953268096     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01346     Document Type: Article

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