Optimization of the in vitro cardiac safety of hydroxamate-based histone deacetylase inhibitors

Journal of Medicinal Chemistry

Volumn 54, Issue 13, 2011, Pages 4752-4772

  Shultz, Michael D ^a   Cao, Xueying ^a   Chen, Christine H ^a   Cho, Young Shin ^a   Davis, Nicole R ^a,b   Eckman, Joe ^a   Fan, Jianmei ^a   Fekete, Alex ^a   Firestone, Brant ^a   Flynn, Julie ^a,c   Green, Jack ^a   Growney, Joseph D ^a   Holmqvist, Mats ^a   Hsu, Meier ^a,d   Jansson, Daniel ^a   Jiang, Lei ^a   Kwon, Paul ^a   Liu, Gang ^a,e   Lombardo, Franco ^a   Lu, Qiang ^a   Majumdar, Dyuti ^a   Meta, Christopher ^a   Perez, Lawrence ^a   Pu, Minying ^a   Ramsey, Tim ^a   Remiszewski, Stacy ^a   Skolnik, Suzanne ^a   Traebert, Martin ^a   Urban, Laszlo ^a   Uttamsingh, Vinita ^a,f   Wang, Ping ^a   Whitebread, Steven ^a   Whitehead, Lewis ^a   Yan Neale, Yan ^a   Yao, Yung Mae ^a   Zhou, Liping ^a   Atadja, Peter ^a   more..

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

^c Alkermes   (United States)

^d MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

^e WUXI APPTEC   (China)

^f Drug Metabolism and Pharmacokinetics   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

(E) 3 (4 [[2 (2 ETHYLPYRAZOLO [1,5 A] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL)N HYDROXY ACRYLAMIDE; (E) 3 (4 [[2 (2 TERT BUTYL 1H PYRROLO [2,3 B] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL)N HYDROXY ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (1H PYRROLO [3,2 B] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL) ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (1H PYRROLO [3,2 C] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (2 METHYLPYRAZOLO [1,5 A] PYRIDIN 3 YL) ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (2 METHYLPYRAZOLO [1,5 A] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (2 PHENYLPYRAZOLO [1,5 A] PYRIDIN 3 YL)ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (6 METHYL 5H PYRROLO [2,3 B] PYRAZIN 7 YL)ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 (4 [[2 (6 METHYL 7H PYRROLO [2,3 D] PYRIMIDIN 5 YL)ETHYLAMINO] METHYL]PHENYL)ACRYLAMIDE; (E) N HYDROXY 3 [4 [(2 IMIDAZO [1,2 A] PYRIDIN 3 YL ETHYLAMINO) METHYL]PHENYL]ACRYLAMIDE; (E) N HYDROXY 3 [4 [([2 [2 (1 HYDROXY 1 METHYL ETHYL) 1H INDOL 3 YL]ETHYL]ISOPROPYLAMINO) METHYL]PHENYL]ACRYLAMIDE; 2 SUBSTITUTED PYRAZOLO [1,5 A] PYRIDIN 3 YLETHYLAMINE DERIVATIVE; 2 TERT BUTYL 1H INDOLE 17F; ANTINEOPLASTIC AGENT; AZATRYPTAMINE DERIVATIVE; BELINOSTAT; CHR 3996; DACINOSTAT; ENTINOSTAT; FLUOROURACIL; GIVINOSTAT; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID; JNJ 26481585; MOCETINOSTAT; ROMIDEPSIN; SB 939; TRYPTAMINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VORINOSTAT;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CARDIOVASCULAR EFFECT; CONTROLLED STUDY; DRUG ACTIVITY; DRUG HALF LIFE; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PHARMACOPHORE; PROCESS OPTIMIZATION; PROTEIN BINDING; QT PROLONGATION; RAT; T CELL LYMPHOMA;

ACRYLAMIDES; ANIMALS; ANTINEOPLASTIC AGENTS; DRUG SCREENING ASSAYS, ANTITUMOR; ETHER-A-GO-GO POTASSIUM CHANNELS; HALF-LIFE; HCT116 CELLS; HISTONE DEACETYLASE INHIBITORS; HUMANS; HYDROXAMIC ACIDS; MICE; MICE, NUDE; MICROSOMES, LIVER; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PATCH-CLAMP TECHNIQUES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION; TRANSPLANTATION, HETEROLOGOUS;

EID: 79960188498     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200388e     Document Type: Article

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