Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors

Journal of Medicinal Chemistry

Volumn 54, Issue 8, 2011, Pages 3051-3064

  Varasi, Mario ^a,b   Thaler, Florian ^b,c   Abate, Agnese ^a,b   Bigogno, Chiara ^d   Boggio, Roberto ^c   Carenzi, Giacomo ^a,b   Cataudella, Tiziana ^a   Dal Zuffo, Roberto ^c   Fulco, Maria Carmela ^a,b   Rozio, Marco Giulio ^d   Mai, Antonello ^e   Dondio, Giulio ^d   Minucci, Saverio ^b,f   Mercurio, Ciro ^a  

^a DAC SRL   (Italy)

^b EUROPEAN INSTITUTE OF ONCOLOGY   (Italy)

^c Congenia SRL ^*  (Italy)

^d NiKem Research   (Italy)

^e SAPIENZA UNIVERSITY OF ROME   (Italy)

^f UNIVERSITY OF MILAN   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOFURAN DERIVATIVE; CHROMAN DERIVATIVE; HISTONE DEACETYLASE; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; N HYDROXY 2 [1' BENZYL 4 OXOSPIRO(CHROMANE 2,4' PIPERIDIN) 6 YL]ACRYLAMIDE; PIPERIDINE DERIVATIVE; SPIRO COMPOUND; UNCLASSIFIED DRUG; ZINC;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CELL CULTURE; CANCER INHIBITION; CANCER MODEL; CELL PROLIFERATION; CONTROLLED STUDY; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CELL LINE, TUMOR; DRUG EVALUATION, PRECLINICAL; HISTONE DEACETYLASE INHIBITORS; HUMANS; HYDROXAMIC ACIDS; MAGNETIC RESONANCE SPECTROSCOPY; MICE; MOLECULAR STRUCTURE; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION;

EID: 79955451248     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200146u     Document Type: Article

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